Anti-cancer Agents In Medicinal Chemistry[JOURNAL]
Sun
200 papers
Comparative Prognosis of HER2-Low versus HER2-Negative Breast Cancer: A Meta-Analysis.
Li Y, Chen T, Tang C … +2 more , Cui H, Li C
Anticancer Agents Med Chem · 2026 Mar · PMID 41833026 · Publisher ↗
With the emergence of new antibody-drug conjugates (ADCs), low human epidermal growth factor receptor (HER2) expression may become a novel treatment target. However, despite the clinical trials of new ADCs, strong eviden...
With the emergence of new antibody-drug conjugates (ADCs), low human epidermal growth factor receptor (HER2) expression may become a novel treatment target. However, despite the clinical trials of new ADCs, strong evidence to prove the practical significance of HER2-low breast cancer (BC) prognosis remains unavailable. </p> Methods: This systematic meta-analysis was undertaken to compare the prognostic value of the survival outcomes of patients with HER2-negative and HER2-low BC. For this, the Cochrane Library and PubMed were searched, and 23 eligible retrospective or prospective studies reporting information related to disease-free survival (DFS), overall survival (OS), and pathological complete response (PCR) rates of patients with HER2- negative and HER2-low BC were included. For both subgroups, the data were pooled using a random-effects model, with hazard ratios (HRs) for OS and DFS and odds ratios (ORs) for PCR, along with their 95% confidence intervals (CIs). OS was the primary endpoint, whereas DFS and PCR rates were the secondary endpoints. </p> Results: We analyzed the 23 studies, which enrolled 781,941 patients with HER2-low BC. OS (HR = 0.82, 95% CI: 0.73-0.92, P = 0.001) significantly improved in patients with HER2-low BC compared with those with HER2-negative BC. However, DFS (HR = 0.87, 95% CI: 0.67-1.12, P = 0.28) did not significantly improve. Furthermore, the PCR rate was lower in patients with HER2-low BC than in patients with HER2-negative BC (OR = 0.88, 95% CI: 0.83-0.93, P < 0.001). </p> Conclusion: Compared with the HER2-negative status, OS is significantly increased, and PCR is significantly decreased in the HER2-low status. However, DFS is not significantly increased.
Taraxasterol Suppresses Renal Cell Carcinoma Progression by Modulating Cell Cycle Progression and Apoptosis.
Xie JG, Liu XC, Han XW … +1 more , Wang YC
Anticancer Agents Med Chem · 2026 Mar · PMID 41833025 · Publisher ↗
Renal cell carcinoma (RCC) is a common and aggressive urological malignancy with limited response to chemotherapy and radiotherapy. The search for effective, low-toxicity natural compounds is therefore of increasing inte...
Renal cell carcinoma (RCC) is a common and aggressive urological malignancy with limited response to chemotherapy and radiotherapy. The search for effective, low-toxicity natural compounds is therefore of increasing interest. Taraxasterol (TAX), a pentacyclic triterpene from dandelion, has shown antitumor activity in several cancers, but its effects on RCC remain unexplored. To investigate the antitumor effects and underlying mechanisms of TAX on RCC in vitro and in vivo. </P> Methods: The human embryonic kidney cell HEK-293T and human RCC cells (786-O) were cultured and treated with different concentrations of TAX (0, 5, 10, and 15 µM), respectively. Next, the MTT assay was employed for detecting cell viability, the scratch assay for cell migration, the Transwell for cell invasion, flow cytometry for changes in mitochondrial membrane potential, apoptosis levels, and cell cycle, and the western blot for protein expression levels related to cell cycle and apoptosis. Additionally, a 786-O xenograft model was established in BALB/c nude mice to evaluate the in vivo antitumor effect of TAX. Tumor volume and weight were measured, and Ki-67 and cleaved Caspase-3 expression in tumor tissues were assessed via immunohistochemistry. </P> Results: TAX did not affect the viability, apoptosis, or cell cycle of HEK-293T cells, but significantly inhibited proliferation, migration, and invasion of 786-O cells, while inducing apoptosis and G2/M arrest in a concentration-dependent manner. TAX reduced mitochondrial membrane potential, increased cleaved-Caspase-3 and cleaved-PARP, decreased Bcl-2, and downregulated Cyclin B1 and CDK1, while upregulating p21 and p27. In vivo, TAX suppressed tumor growth and reduced Ki-67, while increasing cleaved Caspase-3 expression in xenograft tumors. </P> Discussion: These findings support TAX as a promising natural compound for RCC therapy. Further work is needed to validate its effects across additional RCC models and to explore other potential molecular pathways. </P> Conclusion: TAX exerts antiproliferative, pro-apoptotic, and anti-invasive effects on RCC, highlighting its potential as a therapeutic candidate.
Theranostic Potential of [177Lu]Lu-DOTA-Tocilizumab in Multiple Myeloma: A Preclinical Evaluation.
Camacho X, Cabrera M, Perroni C … +6 more , Tassano M, Fernández M, Oddone N, Riva E, Gambini JP, Cabral P
Anticancer Agents Med Chem · 2026 Mar · PMID 41833024 · Publisher ↗
Multiple Myeloma (MM) is a haematological malignancy in which Interleukin-6 (IL-6) plays a crucial role in its growth and spread. The monoclonal antibody Tocilizumab binds strongly to IL-6 receptors, inhibiting their fun...
Multiple Myeloma (MM) is a haematological malignancy in which Interleukin-6 (IL-6) plays a crucial role in its growth and spread. The monoclonal antibody Tocilizumab binds strongly to IL-6 receptors, inhibiting their function. Our aim is to evaluate the potential of [177Lu]Lu-labeled Toclilzumab as a theranostic agent for MM. </P> Methods: Tocilizumab was derivatised with DOTA-NHS ester and radiolabeled with [177Lu]Lu. The stability of the radiochemical compound was evaluated, and in vitro binding and immunoreactive fraction assays were performed. Biodistribution was assessed at 24 and 48 h post-injection (n = 5) in normal and MM-bearing BALB/c nude mice. </P> Results: [177Lu]Lu-DOTA-Tocilizumab remained stable in all tested solutions. Epitope recognition was confirmed by cell-binding studies, and an immunoreactive fraction of 83.7% was observed. In vivo biodistribution studies revealed high tumor uptake over time, with tumor-to-muscle ratios of 11.66 ± 3.81 and 9.54 ± 1.75 at 24 and 48 h, respectively. </P> Discussion: This study focused on the synthesis and characterisation of a new radiolabeled theranostic agent against IL6R, [177Lu]Lu-DOTA-Tocilizumab. This agent demonstrated high radiochemical stability and strong binding to IL-6R in the MM cell line. Biodistribution studies indicated selective retention of the agent in tumor tissue, highlighting its potential for targeted imaging and therapy in IL-6R-positive cancers and paving the way for future research into its application in related diseases. </P> Conclusions: [177Lu]Lu-DOTA-Tocilizumab represents a potential theranostic agent for MM. Therefore, we expect this agent to open the way to new diagnostic and therapeutic strategies for this devastating disease.
The Role of Artemisinin and its Derivatives in Cancer Therapy via Ferroptosis: A Systematic Review of In Vitro, In Vivo, and In Silico Studies.
Osmanlioglu Dag SR, Tatli Cankaya II, Ozkan AMG
Anticancer Agents Med Chem · 2026 Mar · PMID 41833023 · Publisher ↗
Artemisinin (ART), a sesquiterpene lactone derived from Artemisia annua L., and its semisynthetic derivatives such as dihydroartemisinin (DHA) and artesunate (ARTE) have gained significant attention for their anticancer...
Artemisinin (ART), a sesquiterpene lactone derived from Artemisia annua L., and its semisynthetic derivatives such as dihydroartemisinin (DHA) and artesunate (ARTE) have gained significant attention for their anticancer potential beyond their established antimalarial effects. The antitumor activity is mediated by various mechanisms, with ferroptosis-an iron-dependent, non-apoptotic form of cell death characterized by lipid peroxidation-standing out as a key pathway. Recent in vitro, in vivo, and in silico studies suggest that artemisinin compounds can trigger ferroptosis in various cancers, including breast, liver, pancreatic, and glioma, by disrupting iron homeostasis, inhibiting glutathione peroxidase 4 (GPX4), and increasing reactive oxygen species (ROS) accumulation. </P> Methods: A comprehensive literature search was conducted up to 2025 using relevant keywords related to artemisinin, cancer, and ferroptosis in databases such as PubMed, Web of Science, and Scopus. </P> Results: Experimental studies demonstrate that dihydroartemisinin and artesunate elevate intracellular Fe²⁺ levels and promote ROS-mediated lipid peroxidation. Animal models further validate these effects, showing tumor growth suppression with minimal systemic toxicity. In silico analyses support these findings, revealing interactions between artemisinin derivatives and ferroptosis-related proteins like GPX4 and transferrin receptor 1 (TfR1). </P> Discussion: The findings collectively indicate that artemisinin and its derivatives induce ferroptosis through irondependent ROS accumulation and GPX4 inhibition, positioning ferroptosis as a central mechanism underlying their anticancer activity. </P> Conclusion: This review analyzed 66 original research articles and identified ferroptosis as the primary mechanism by which artemisinin and its derivatives exert anticancer effects, often in combination with apoptosis, autophagy, or cell cycle arrest. In silico studies confirm strong interactions with ferroptosis-related targets. Lung and liver cancers emerged as the most frequently studied and responsive, highlighting them as key targets for future translational efforts. Standardized methodologies are needed to improve reproducibility and clinical relevance.
Thiourea Derivatives for the Potential Treatment of Lung Cancer via the Inhibition of EGFR and Efflux Pumps: Synthesis, In Silico, and In Vitro Studies.
Abu-Zaid R, Abusara OH, Hussein B … +2 more , Saqallah FG, Albujuq NR
Anticancer Agents Med Chem · 2026 Mar · PMID 41833022 · Publisher ↗
INTRODUCTION: The overexpression and/or mutations of Epidermal Growth Factor Receptor (EGFR) are associated with the progression of several cancers. Thiourea derivatives have emerged as promising compounds to target EGFR...
INTRODUCTION: The overexpression and/or mutations of Epidermal Growth Factor Receptor (EGFR) are associated with the progression of several cancers. Thiourea derivatives have emerged as promising compounds to target EGFR for cancer treatment. METHODS: Ten thiourea derivatives (1-10) underwent virtual screening, were synthesized, and evaluated on EGFR-expressing cells and normal fibroblasts. RESULTS AND DISCUSSION: Compound 3 had the highest binding affinity towards HER1 and HER2 (EGFR family) with the Lowest Binding Energy (LBE) values of -9.6 and -10.9 kcal/mol, respectively. Against lung cancer cells, H69 and H2073 cells, compound 3 had IC50 values of 3.68 and 2.48 μM, respectively, with a selectivity index greater than 25 on both cancer cells. A combination index value of 1.0 (additive effect) was achieved on both cell lines when compound 3 was combined with Doxorubicin (DOX). The cytotoxic effect of compound 3 may also be driven via a non-mitochondrial pathway, as elucidated by the JC-1 mitochondrial assay. The enhancement of DOX toxicity against H69 cells (initial IC50 value was 0.6 μM) by the addition of 0.1 and 1 μM of compound 3 to reach an IC50 values of 0.27 and 0.04 μM, respectively, may be driven via the inhibitory effect of compound 3 on efflux pumps, such as ABCC1 and RALBP1 (LBE values of -9.2 and -8.41 kcal/mol, respectively), known as reasons for DOX resistance and their expression in H69 cells. CONCLUSION: Compound 3 has shown to have cytotoxic effects against EGFR-expressing lung cancer cells, causes an additive effect with conventional chemotherapy, and may be used to treat multi-drug-resistant cancers.
Apoptotic and Anti-Proliferative Potential of Spirulina platensis Methanolic Extract Against the Human Breast Cancer Cell Line MDA-MB-231: A Step Towards Functional Cancer Therapy.
Srivastava A, Siddiqi Z, Siddiqui S … +1 more , Ahmad R
Anticancer Agents Med Chem · 2026 Mar · PMID 41833021 · Publisher ↗
INTRODUCTION: Algae have garnered increasing interest in the fields of medicine and nutrition as a source of nutritious and non-toxic healthcare supplements. Spirulina platensis (SP), a microalga and a welldocumented nut...
INTRODUCTION: Algae have garnered increasing interest in the fields of medicine and nutrition as a source of nutritious and non-toxic healthcare supplements. Spirulina platensis (SP), a microalga and a welldocumented nutritional supplement, is recognized for its high medicinal value and potential anticancer properties. The present study evaluated the apoptosis-inducing effect of methanolic extract of Spirulina platensis (SPM) on human breast cancer MDA-MB-231 cells. METHODS: The extract was prepared using standard methanol extraction techniques. Cytotoxicity was assessed using the MTT assay over varying concentrations and time intervals. Morphological changes were observed under a phase-contrast microscope. Apoptosis was further confirmed through acridine orange/ ethidium bromide (AO/EB) dual staining and DNA fragmentation analysis. The effect of SPM on normal HEK-293 cells was also evaluated to determine its selectivity and safety profile. RESULTS: HPLC analysis identified C-phycocyanin (C-PC) as the major bioactive phytoconstituent in the SPM extract. The extract showed antioxidant activity and dose- and time-dependent growth inhibition of MDA-MB-231 cells (IC50: 3433 μg/mL). Treated cells displayed apoptotic morphology under a phasecontrast microscope and late apoptosis at higher doses, confirmed by AO/EB staining. DNA fragmentation was observed in MDA-MB-231 cells but not in HEK-293 cells, which showed minimal cytotoxicity (IC₂⁽: 7250 μg/mL). DISCUSSION: The presence of C-PC most likely contributes to the extract's antioxidant and anticancer effects. SPM selectively induced apoptosis and inhibited proliferation in MDA-MB-231 cells, with a negligible impact on normal cells, highlighting its potential as a safe and natural anticancer candidate. CONCLUSION: As evident from the results, SPM extract has demonstrated potential for its clinical applications in cancer therapy as an adjunct to the main line of treatment, provided that further studies are carried out on other cancer cell lines and animal models in future.
Aptamers in Osteosarcoma: New Paths for Diagnosis and Treatment.
Awad G, Boutros M, Chartouni A … +1 more , Pretell-Mazzini J
Anticancer Agents Med Chem · 2026 Mar · PMID 41820318 · Publisher ↗
INTRODUCTION: Osteosarcoma remains the most common primary malignant bone tumor, with poor outcomes in metastatic or recurrent cases. Current treatments often fail to prevent relapse, highlighting the need for innovative...
INTRODUCTION: Osteosarcoma remains the most common primary malignant bone tumor, with poor outcomes in metastatic or recurrent cases. Current treatments often fail to prevent relapse, highlighting the need for innovative therapeutic strategies. Aptamers, short and single-stranded oligonucleotides capable of folding into three-dimensional shapes, have emerged as promising tools for targeted cancer diagnostics and therapy due to their high affinity, specificity, and modifiability. METHODS: A structured search was conducted through PubMed, Scopus, and Google Scholar up to March 2025, focusing on peer-reviewed articles exploring the use of aptamers in osteosarcoma. A total of 158 studies were included, highlighting aptamer applications in tumor diagnosis, pathway targeting, and precision drug delivery. RESULTS: Aptamers demonstrated significant potential in osteosarcoma research, notably in identifying tumorigenesis pathways, enhancing diagnostic accuracy through ELISA and biosensors, and improving targeted drug delivery. SELEX-derived aptamers effectively targeted molecules such as CD133, EGFR, VEGFA, and FGFR1, leading to enhanced cytotoxicity, reduced off-target effects, and greater specificity for osteosarcoma cells and cancer stem cells. The integration of aptamers with nanoparticles further optimized therapeutic delivery, highlighting their capability to enhance precision medicine in osteosarcoma. DISCUSSION: Aptamers offer clear benefits over traditional osteosarcoma treatments. Their strong binding affinity to cancer cells, low risk of immune reactions, and flexible chemical modifications make them powerful tools for diagnosis and therapy, especially when combined with nanoparticle delivery systems. CONCLUSION: Aptamers represent a promising class of targeted agents for osteosarcoma. Future research should prioritize optimizing delivery strategies and validating clinical efficacy to accelerate their integration into clinical practice.
Cancer Stem Cells and Medicinal Plants, A Comprehensive Review of their Potential in Tumor Suppression and Recurrence Prevention.
Javazmi RF, Hosseini SA, Bagheri SM
Anticancer Agents Med Chem · 2026 Mar · PMID 41787995 · Publisher ↗
INTRODUCTION: Cancer Stem Cells (CSCs) drive tumor initiation, progression, and recurrence due to their self-renewal and differentiation capacities. Herbal medicines offer potential for targeting CSCs by disrupting key p...
INTRODUCTION: Cancer Stem Cells (CSCs) drive tumor initiation, progression, and recurrence due to their self-renewal and differentiation capacities. Herbal medicines offer potential for targeting CSCs by disrupting key pathways, inducing apoptosis, and enhancing the efficacy of conventional therapy. This review evaluates the effectiveness of plant-based compounds in suppressing CSCs across various cancers. METHODS: A systematic search was conducted across databases (ISI Web of Science, PubMed, ScienceDirect, Scopus, Biological Abstracts, Chemical Abstracts) up to March 2025, using keywords such as "cancer stem cells and plant extracts." Inclusion criteria were English-language original articles or reviews on plant-based compounds targeting CSCs (in vitro, in vivo, or clinical studies) with full-text availability. Duplicates, non-relevant, non-English, or abstract-only studies were excluded, yielding 43 studies. RESULTS: Herbal medicines derived from plants such as Pao Pereira, Rauwolfia vomitoria, and Celastrus orbiculatus inhibit CSC proliferation, self-renewal, and chemoresistance across breast, colon, pancreatic, gastric, ovarian, prostate, glioblastoma, hepatic, and lung cancers. Mechanisms include disruption of the TGF-β/Smad pathway, induction of apoptosis via caspase activation, and ROS-mediated oxidative stress, with compounds such as curcumin and resveratrol targeting Wnt, Notch, and Hedgehog pathways. DISCUSSION: Plant-derived compounds show promise in targeting CSCs, enhancing chemotherapy sensitivity, and reducing tumor recurrence. However, inconsistent potency, limited clinical data, and bioavailability challenges limit translation. Standardized extracts and rigorous clinical trials are needed to validate efficacy and safety. CONCLUSION: Herbal medicines offer a promising complementary approach to CSC-targeted cancer therapy, but further research is essential to overcome current limitations and enable clinical integration.
Fish-Derived Antimicrobial Peptides (AMPs) as Anticancer Agents: A Mini-Review of In Vitro Evidence.
Mohd Noordin MA, Najm AA, Dyari HRE … +2 more , Law D, Fazry S
Anticancer Agents Med Chem · 2026 Mar · PMID 41787994 · Publisher ↗
INTRODUCTION: Marine fish provide a significant reservoir of Antimicrobial Peptides (AMPs) with potential anticancer properties, an area of growing scientific focus. METHODOLOGY: This review gathers findings from studies...
INTRODUCTION: Marine fish provide a significant reservoir of Antimicrobial Peptides (AMPs) with potential anticancer properties, an area of growing scientific focus. METHODOLOGY: This review gathers findings from studies published between 2020 and 2024, sourced from databases such as Google Scholar, Scopus, BioMed Central, and ScienceDirect, identifying 15 relevant research papers highlighting the potential of fish-derived antimicrobial peptides in anticancer research. RESULT: AMPs exhibit broad-spectrum anticancer activity against diverse cancer cell lines, primarily by inducing apoptosis or necrosis through mechanisms that involve ROS generation, mitochondrial dysfunction, and DNA damage. DISCUSSION: The therapeutic promise of fish AMPs is rooted in their diverse mechanisms, including highly selective cytotoxicity and the ability to exploit oxidative stress and trigger irreversible cell death, along with antiangiogenic properties. Future clinical development requires synthetic optimization and advanced drug delivery systems to enhance stability, bioavailability, and targeted delivery. CONCLUSION: This study highlights the promise of fish antimicrobial peptides as an additional class of anticancer therapies and explores future prospects, including improvements in drug administration and peptide modification, that might enhance their clinical application.
Bevacizumab and Fingolimod Combination Therapy Induce Cytotoxicity and Apoptosis in Ovcar-3 Cells.
Bayirli R, Yıldız Eren C
Anticancer Agents Med Chem · 2026 Feb · PMID 41764608 · Publisher ↗
INTRODUCTION: Ovarian cancer remains one of the fatal gynecological malignancies. Bevacizumab is a monoclonal antibody targeting vascular endothelial growth factor. Fingolimod has recently garnered attention as a potenti...
INTRODUCTION: Ovarian cancer remains one of the fatal gynecological malignancies. Bevacizumab is a monoclonal antibody targeting vascular endothelial growth factor. Fingolimod has recently garnered attention as a potential anticancer compound. Emerging evidence highlights the advantages of combinatorial treatment approaches in ovarian cancer. This study aims to investigate the cytotoxic and pro-apoptotic effects of the combination therapy involving Bevacizumab and Fingolimod in Ovcar-3 cells. By elucidating the molecular mechanisms underlying their potential synergistic interactions, this research seeks to provide valuable insights into novel therapeutic strategies for ovarian cancer treatment. METHODS: Ovcar-3 cells were obtained from the American Type Culture Collection. The concentrations of Bevacizumab and Fingolimod between 100-3.125 μM were added to Ovcar-3 cells. MTT, annexin-V staining, caspase 3/7 activation, mitochondrial potential, and reactive oxygen species analyses were performed. RESULTS: The Bevacizumab-Fingolimod combination triggered apoptosis at 21.79%. The viability was decreased to 78.20%. The percentage of early apoptotic cells was 18.67%, and 3.12% of late apoptotic cells was found to be 3.12%. The Bevacizumab-Fingolimod combination activated caspase 3/7 in Ovcar-3 cells after 24 hours of treatment. The Bevacizumab-Fingolimod combination changed the polarization of mitochondria of Ovcar-3 cells. DISCUSSION: Our study confirmed that Bevacizumab monotherapy significantly reduced the viability of Ovcar-3 cells, demonstrating its antiproliferative effects. These findings support previous results. When Bevacizumab was combined with Fingolimod, its efficacy was further enhanced, as indicated by high apoptotic rates. CONCLUSION: The combination of Bevacizumab and Fingolimod presents a promising treatment strategy for ovarian cancer.
Investigation of the Immunomodulatory Effect of Quinoline Derivatives with Antitumor Activity.
Jaber MA, Al-Sheikh A, Abu Oun M … +1 more , Abuarqoub D
Anticancer Agents Med Chem · 2026 Feb · PMID 41755408 · Publisher ↗
INTRODUCTION: In the last two decades, quinoline derivatives have garnered significant attention for their anticancer and immunomodulatory properties. These compounds have shown potential in modulating inflammatory respo...
INTRODUCTION: In the last two decades, quinoline derivatives have garnered significant attention for their anticancer and immunomodulatory properties. These compounds have shown potential in modulating inflammatory responses, which are often implicated in cancer progression. This study aimed to evaluate the immunomodulatory effects and anti-migratory properties of three novel quinoline derivatives in THP-1-derived macrophage-like cells. METHODS: Macrophage-like cells derived from the THP-1 cell line were treated with three quinoline derivatives (3c, 3d, and 3e). The expression levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and the antiinflammatory cytokine IL-10 were measured. Additionally, the compounds' effects on the expression of migration- related genes and their ability to inhibit cell migration were assessed. RESULTS: Treatment with quinoline derivatives led to a significant reduction in TNF-α, IL-1β, and IL-6 expression, particularly with compounds 3c and 3d. In contrast, compound 3e induced a weaker response in proinflammatory cytokine suppression but notably elevated IL-10 levels. Furthermore, all three compounds demonstrated concentration-dependent inhibition of cell migration, with compound 3c showing the most substantial effect and pronounced changes in migration-related gene expression. DISCUSSION: The tested quinoline derivatives exhibit promising immunomodulatory and anti-migratory activities. Compound 3c, in particular, emerged as a strong candidate for further investigation due to its robust antiinflammatory and migration-inhibitory effects. CONCLUSION: These findings highlight the therapeutic potential of quinoline derivatives in managing inflammation- associated cancer progression.
Phytosynthesis of Selenium Nanoparticles from Morus rubra (L.) and Evaluation of its Bioactive Potential: Antioxidant, Antimicrobial, and Anticancer.
Rocha LVM, R L, S MB … +2 more , A HJ, Rani I JC
Anticancer Agents Med Chem · 2026 Feb · PMID 41716055 · Publisher ↗
INTRODUCTION: Selenium, a trace element with vital antioxidant and cancer-preventive properties, poses toxicity risks at higher doses, which can be mitigated through the green synthesis of nanoparticles using plant phyto...
INTRODUCTION: Selenium, a trace element with vital antioxidant and cancer-preventive properties, poses toxicity risks at higher doses, which can be mitigated through the green synthesis of nanoparticles using plant phytochemicals as natural reducing and stabilizing agents. This study aimed to investigate the potential of Morus rubra (L.) leaf extract as an effective natural reducing agent for the green synthesis of selenium nanoparticles, with an emphasis on their chemical characterization and assessment of biological activities. METHODS: The synthesized SeNPs were characterized using UV-Vis spectroscopy, FTIR, XRD, and TEM. Antimicrobial activity was evaluated using the agar well diffusion method, and MIC was determined by broth microdilution assay. Cytotoxic effects were assessed using the MTT assay, and apoptosis was evaluated using AO/EB dual staining. RESULTS: An absorption peak at 275 nm confirmed successful SeNP biosynthesis, yielding 10-60 nm crystalline nanoparticles. The SeNPs exhibited potent antioxidant activity (IC50 56.12 μg/mL), strong antimicrobial effects (largest inhibition 24 mm for B. subtilis; MIC 50-80 μg/mL), and selective cytotoxicity against MDA-MB-231 cancer cells (IC50 23.09 μg/mL), with higher tolerance in normal cells (IC50 50.16 μg/mL). AO/EB staining indicated that 70-80% of treated cancer cells underwent apoptosis. DISCUSSION: These findings indicate that Morus rubra-mediated selenium nanoparticles align with recent advances in green nanotechnology, where plant extracts enhance both the safety and functional performance of nanoparticles. CONCLUSION: The biosynthesized selenium nanoparticles using Morus rubra leaf extract demonstrated efficient antioxidant, antimicrobial, and selective anticancer activities, highlighting their promising potential for biomedical applications.
Natural Combatants: How Herbal Monomers Regulate Autophagy in Ovarian Cancer.
Gao M, Zhu Y, Yu Y … +3 more , Ding D, Wang Y, Han F
Anticancer Agents Med Chem · 2026 · PMID 41691674 · Full text
INTRODUCTION: Ovarian cancer (OC) is a lethal gynecological malignancy, with current therapies constrained by drug resistance and side effects. Autophagy plays a dual role in OC, while Traditional Chinese Medicine (TCM)...
INTRODUCTION: Ovarian cancer (OC) is a lethal gynecological malignancy, with current therapies constrained by drug resistance and side effects. Autophagy plays a dual role in OC, while Traditional Chinese Medicine (TCM) monomers, as natural bioactive compounds, demonstrate significant potential in regulating autophagy and combating tumors. This review aims to summarize the mechanisms by which TCM monomers regulate autophagy in OC, providing a theoretical basis for TCM-based drug development and clinical applications. METHODS: Relevant literature was retrieved from databases including PubMed, Web of Science, and CNKI. The action targets and signaling pathways of TCM monomers were summarized to elucidate their mechanisms in regulating OC autophagy. RESULTS: TCM monomers (e.g., ginsenoside Rg3, curcumin) bidirectionally regulate OC autophagy through pathways such as PI3K/AKT/mTOR and MAPK; some enhance chemotherapy sensitivity by inducing excessive autophagy or inhibiting protective autophagy. DISCUSSION: TCM monotherapy offers unique advantages in the treatment of OC through precise regulation of autophagy. However, most studies are limited to in vitro experiments, and there is insufficient in vivo efficacy and clinical translational evidence. CONCLUSION: Validating the complex action network of TCM monomers through multi-omics and clinical studies, and exploring their synergistic effects with conventional chemotherapy, is crucial for advancing the development of natural anti-ovarian cancer drugs.
Hydrazones as Potential Antimelanoma Prototypes: A Systematic and Patent Review.
Macêdo BVS, Macedo ES, Diniz MC … +1 more , Mendes RL
Anticancer Agents Med Chem · 2026 Feb · PMID 41664366 · Publisher ↗
<p> Introduction: Hydrazones are chemical compounds with the potential to inhibit various neoplasms, including melanoma, a highly metastatic and multidrug-resistant cancer. This study aimed to systematically review the l...
<p> Introduction: Hydrazones are chemical compounds with the potential to inhibit various neoplasms, including melanoma, a highly metastatic and multidrug-resistant cancer. This study aimed to systematically review the literature and analyze patents to assess the potential of hydrazones as prototype anti-melanoma agents. </p><p> Methods: Following PRISMA guidelines (OSF registration: DOI 10.17605/OSF.IO/3AWR9), a systematic search was conducted in PubMed/Medline, Web of Science, ScienceDirect, and Scopus for studies published from January 2019 to February 2024 using the terms "hydrazone" and "melanoma". Only original Englishlanguage studies with experimental evaluation of anti-melanoma activity, in vitro and/or in vivo, were included. Patent searches were also carried out in ESPACENET, WIPO, LENS, and Google Patents using the IPC code A61P35/00. </p><p> Results: From 1,072 records, 35 articles met eligibility criteria. All studies reported in vitro anti-melanoma activity of hydrazones; however, none included in vivo assays. N-acylhydrazones were the most frequently investigated subclass, featured in 19 studies. The patent analysis identified 41 filings using the combined terms "hydrazone AND melanoma", with Google Patents accounting for the majority (29 filings). </p><p> Discussion: Hydrazones, particularly N-acylhydrazones, showed significant in vitro activity and selectivity, surpassing traditional drugs like cisplatin in some cases. The limited number of patent filings might indicate difficulties with protecting intellectual property, including effects from the COVID-19 pandemic. However, methodological differences and the lack of in vivo data are still major challenges. This emphasizes the need for more consistent and applicable research. </p><p> Conclusion: Despite their potential, further studies are needed to validate hydrazones as a distinct class of antineoplastic agents.
Lapatinib Promotes Apoptosis in Hepatoma Cells by Regulating SPP1 Expression.
Wang D, Jiang K, Feng H … +4 more , Zhang L, Li D, Fu S, Sun Y
Anticancer Agents Med Chem · 2026 Jan · PMID 41664365 · Publisher ↗
<P> Introduction: Lapatinib, a novel targeted anti-tumor drug in clinical use, demonstrates notable potential for liver cancer treatment. However, its mechanism of action in liver hepatocellular carcinoma (LIHC) remains...
<P> Introduction: Lapatinib, a novel targeted anti-tumor drug in clinical use, demonstrates notable potential for liver cancer treatment. However, its mechanism of action in liver hepatocellular carcinoma (LIHC) remains poorly understood. This investigation sought to clarify the function of secreted phosphoprotein 1 (SPP1) in LIHC and investigate the anti-tumor effects of lapatinib on SPP1 expression. </P> <P> Methods: We analyzed data from normal liver and LIHC specimens obtained from The Cancer Genome Atlas (TCGA) and the GSE6764 dataset using R version 4.2.1. SPP1 protein expression in LIHC patients and its impact on patient prognosis were evaluated. Western blotting evaluated lapatinib-induced alterations in SPP1 protein levels in hepatoma cells. Cell Counting Kit-8 (CCK-8) assays measured lapatinib's impact on hepatoma cell growth and proliferation. </P> <P> Results and Discussion: SPP1 level was notably elevated in LIHC specimens versus normal liver tissues (P < 0.01). The survival outcomes were notably inferior in cases displaying elevated SPP1 levels versus those with reduced levels (P < 0.05). CCK-8 analyses demonstrated that a decrease in SPP1 expression leads to a significant inhibition of growth and proliferation in the LIHC cell line HepG2, while lapatinib can inhibit the survival of liver cancer cells. Western blotting analyses revealed that lapatinib treatment reduced SPP1 expression in HepG2 cells, increased the ratio of BAX/Bcl2, and triggered apoptosis in cells. </P> <P> Conclusion: These observations demonstrate that the expression of SPP1 is associated with disease progression and survival in patients with LIHC. Lapatinib exerts its anti-tumor effects in LIHC by downregulating SPP1 expression and promoting apoptosis in hepatoma cells.
Comprehensive Biochemical Insights into Prostate-Specific Antigen: From Biomarker to Functional Mediator in Prostate Cancer Pathophysiology.
Das L
Anticancer Agents Med Chem · 2026 Jan · PMID 41588903 · Publisher ↗
Prostate-Specific Antigen (PSA) is a glycoprotein produced in the prostate and is widely used as a biomarker for the diagnosis of prostate cancer (PCa). Although elevated PSA levels are often associated with PCa, several...
Prostate-Specific Antigen (PSA) is a glycoprotein produced in the prostate and is widely used as a biomarker for the diagnosis of prostate cancer (PCa). Although elevated PSA levels are often associated with PCa, several noncancerous conditions can also lead to increased PSA. In addition to total PSA, various PSA isoforms are detectable in the blood of patients, and their levels may differ depending on the underlying pathophysiological condition, whether benign or malignant. Measuring serum PSA levels alone is not sufficient to detect PCa, leading to widespread overdiagnosis and overtreatment. Therefore, comprehensive biochemical insights into PSA and its isoforms, of normal, benign, and malignant origin, may improve PSA assays for PCa diagnosis. Apart from its role as a biomarker, PSA plays multiple roles in the pathophysiology of PCa by activating the Epithelial-Mesenchymal Transition (EMT) and promoting tumor progression, as well as regulating the invasion and metastasis of PCa cells. In PCa, elevated PSA levels are associated with immunosuppression, antiapoptotic properties, and inhibition of angiogenesis. A comprehensive review of numerous important research findings on PSA and its isoforms was conducted to elucidate the role of PSA as a biomarker and functional mediator in PCa pathophysiology. Thus, the use of PSA as a biomarker for the diagnosis of PCa can minimize unnecessary and inappropriate biopsies, identify suitable patients for prostate biopsy, ensure early diagnosis, and initiate treatment at an early stage of PCa. Furthermore, the role of PSA as a functional mediator will enable us to study the pathophysiology of patients with prostate cancer (PCa).
An Overview of the Antioxidant, Anti-inflammatory, and Anticancer Effects of Statins.
Zarei F, Salimi Z, Zeinivand M … +2 more , Zamani N, Bahrani R
Anticancer Agents Med Chem · 2026 · PMID 41588902 · Publisher ↗
INTRODUCTION: Statins are a class of cholesterol-lowering agents widely used in clinical practice to reduce plasma levels of low-density lipoprotein cholesterol in hyperlipidemic patients. Beyond their lipidlowering role...
INTRODUCTION: Statins are a class of cholesterol-lowering agents widely used in clinical practice to reduce plasma levels of low-density lipoprotein cholesterol in hyperlipidemic patients. Beyond their lipidlowering roles, statins exhibit several additional effects. METHODS: In the current review, we searched PubMed, ScienceDirect, and Google Scholar databases using the keywords "Statins," "HMG-CoA reductase inhibitors," "Anti-inflammatory," "Antioxidant," and "Anticancer" to provide an overview of the effects of statins. Articles published on these topics between 1990 and 2025 were included. The retrieved records were imported into EndNote, and duplicates were removed. RESULT: Multiple potential therapeutic benefits of statins have been described, including suppression of apoptosis, antioxidant, anti-inflammatory and anticancer effects, immunomodulation and neuroprotection. DISCUSSION: NADPH oxidases (NOX) play a crucial role in the development of various diseases through excessive production of reactive oxygen species (ROS) and the creation of oxidative stress conditions. Stimulation of BDNF/Nrf2, inhibition of NOX pathways, and reduction of intracellular ROS via enhanced antioxidant activity represent possible mechanisms through which statins exert their effects. Interestingly, ROS and inflammatory cytokines activate nuclear factor kappa B (NF-κB), a critical factor in the development of malignant tumors, which induces the expression of genes involved in cell proliferation and carcinogenesis. Furthermore, statins inhibit NF-κB activity, a key transcriptional regulator in inflammatory responses. CONCLUSION: Clinical evidence suggests that statins may reduce the risk of various cancers and disease recurrence due to their anti-inflammatory and antioxidant properties. These findings form the basis for new therapeutic avenues in cancer treatment, potentially offering a more promising strategy than statin monotherapy.
Signalling Pathways and Inhibitors in Triple Negative Breast Cancer: Current Progress.
Das A, Lather V
Anticancer Agents Med Chem · 2026 · PMID 41588901 · Publisher ↗
INTRODUCTION: Triple Negative Breast Cancer (TNBC), which makes up 15% of all breast cancers, is widely acknowledged as the most aggressive and challenging subtype of the disease. It is characterized by the absence of HE...
INTRODUCTION: Triple Negative Breast Cancer (TNBC), which makes up 15% of all breast cancers, is widely acknowledged as the most aggressive and challenging subtype of the disease. It is characterized by the absence of HER2 receptors, progesterone, and estrogen, which limits the options for targeted treatment and mainly affects younger women. It is associated with a poor prognosis due to its rapid progression, high recurrence rates, and risk of metastasizing into vital organs like the brain and lungs. These clinical challenges underscore the urgent need for personalized treatment plans and innovative therapeutic strategies. METHODS: Numerous studies have identified dysregulated signaling pathways in TNBC, including the PI3K/AKT/mTOR, JAK/STAT, Wnt/β-catenin, Notch, and MAPK/ERK pathways, which offer therapeutic targets. RESULTS: Recent developments in clinical and molecular research have presented potential treatment strategies. Pembrolizumab and other immune checkpoint inhibitors have demonstrated significant benefits when used in conjunction with chemotherapy for both early-stage and metastatic TNBC. In advanced patients, sacituzumab, govitecan, and other Antibody-Drug Conjugates (ADCs) have shown remarkable efficacy in delivering cytotoxic medications, improving progression-free survival. Significant obstacles still exist despite these developments, such as tumor heterogeneity and treatment resistance. DISCUSSION: This review highlights the beneficial effects of small molecule inhibitors and combination therapies in treating the deadliest type of breast cancer, as well as the therapeutic potential of targeting dysregulated signaling pathways and providing insight into potential avenues for developing new therapies. CONCLUSION: To significantly enhance outcomes for TNBC patients, future research must concentrate on identifying predictive biomarkers and refining individualized therapy plans.
Green Synthesis of L.-derived Silver Nanoparticles: Evaluation of Antioxidant, Antibacterial, and Anticancer Potential against Triple-Negative Breast Cancer Cells.
Abdullateef A, Unegbu IA, Halilu EM
Anticancer Agents Med Chem · 2026 · PMID 41588900 · Publisher ↗
INTRODUCTION: Mentha spicata L. (Lamiaceae) has been used in traditional medicine to cure indigestion, stomach aches, and diarrhea. This research aims to synthesize silver nanoparticles from aqueous extract of M. spicata...
INTRODUCTION: Mentha spicata L. (Lamiaceae) has been used in traditional medicine to cure indigestion, stomach aches, and diarrhea. This research aims to synthesize silver nanoparticles from aqueous extract of M. spicata and to investigate its antioxidant, antibacterial, and anticancer activities. METHODS: The plant was extracted using maceration with water, and Mentha spicata-silver nanoparticles (MAgNPs) were prepared using a 5 mM silver nitrate solution. The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide scavenging assays. Antibacterial analysis was done through the agar disk diffusion method. The anticancer potential was evaluated using the cytotoxicity and MTT assays. RESULTS: The phytochemical screening revealed the presence of flavonoids and other phenolic compounds. The aqueous extract and silver nanoparticles scavenged the DPPH and hydrogen peroxide free radicals, with IC50 values of 1.556 mg/mL and 1.695 mg/mL, respectively. The bacterial strains were susceptible to the extract and silver nanoparticles, with inhibitory zones ranging from 4 to 11 mm. The zeta analysis revealed a size of 70.08 nm and a potential of -13.17 mV. The XRD showed a crystalline structure of silver nanoparticles. The FTIR revealed a characteristic N-H stretching frequency. The extract and nanoparticles exhibited cytotoxic and anti-proliferative effects in vitro against MDA-MB-231 cancer cells, with a significant difference among means (p < 0.05). DISCUSSION: There is an urgent need to screen and standardize medicinal plants with medicinal benefits and less toxicity, which also serve as chelating agents in drug delivery. CONCLUSION: The ability of the extract to scavenge free radicals and inhibit bacterial growth may be due to its chemical constituents. MAgNPs may be a viable option for potential application and development in cancer therapy.
A Needle in a Haystack: The Precision of Liquid Biopsy in Finding Bone Tumors.
Nohra A, Awad G, El Khoury JV … +1 more , Boutros M
Anticancer Agents Med Chem · 2026 Jan · PMID 41582380 · Publisher ↗
INTRODUCTION: Bone tumors, especially in advanced stages, pose serious diagnostic and therapeutic challenges due to their aggressive nature and the invasiveness of traditional biopsy techniques. Liquid biopsy offers a pr...
INTRODUCTION: Bone tumors, especially in advanced stages, pose serious diagnostic and therapeutic challenges due to their aggressive nature and the invasiveness of traditional biopsy techniques. Liquid biopsy offers a promising, minimally invasive alternative by analyzing tumor-derived components from bodily fluids, such as circulating tumor cells (CTCs), circulating tumor DNA (ctDNA), and extracellular vesicles (EVs). These biomarkers enable dynamic and precise disease monitoring. OBJECTIVE: This review aimed to investigate the role of liquid biopsy in the diagnosis, prognosis, and treatment guidance of bone tumors, highlighting recent molecular advances and clinical findings. METHODS: A structured narrative review was conducted using PubMed, covering studies published up to July 2024. Studies involving osteosarcoma, Ewing sarcoma, chondrosarcoma, and chordoma were included, focusing on the clinical implications of CTCs, ctDNA, and EVs from plasma, serum, and other fluids. RESULTS: Liquid biopsy technologies demonstrated high diagnostic accuracy in bone tumors. In osteosarcoma, CTC detection using qRT-PCR and FISH methods showed sensitivities up to 98.6% and was strongly associated with metastatic disease and recurrence risk. ctDNA profiling identified tumor-specific mutations, hypomethylation markers (e.g., IRX1), and early relapse indicators with up to 97.4% specificity. EV-associated biomarkers, particularly miRNAs, such as miR-25-3p and a 3-miRNA signature, distinguished tumor subtypes and predicted metastasis-free survival. Advanced techniques, like SERS and MALDI-TOF MS profiling of exosomes, achieved diagnostic accuracies near 100%. EV RNA sequencing revealed differential gene expression and fusion events linked to metastatic progression and long-term outcomes. CONCLUSION: Liquid biopsy holds strong potential for transforming bone tumor care. Its clinical adoption depends on further validation through standardized methods and large-scale studies.
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