J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41493169
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HIF2α is aberrantly upregulated in some renal cell carcinomas due to VHL mutations, supporting HIF2α inhibition as a compelling therapeutic approach for such cases. Therefore, the six compounds (designated as Compounds 1...HIF2α is aberrantly upregulated in some renal cell carcinomas due to VHL mutations, supporting HIF2α inhibition as a compelling therapeutic approach for such cases. Therefore, the six compounds (designated as Compounds 1-6) were screened from the Maybridge database based on the constructed pharmacophore model and molecular docking. Subsequently, the docking models of Compounds 1-6 with HIF2α were analysed. Affinity assays revealed that both Compound-4 and Compound-5 exhibited robust affinity towards human recombinant HIF2α. MD simulations displayed that Compound-4 and Compound-5 stably bound to the active pocket of HIF2α. Cell experiments demonstrated that Compound-4 effectively inhibited the growth of the 786-O human renal cell carcinomas line (IC = 1.35 ± 0.06 μM). This study demonstrates that Compound-4 may serve as a potential candidate compound for renal cell carcinomas therapy.
Di Rienzo A, Faris A, Mingoia M
… +8 more, Conte C, Marinucci L, Magi G, Cufaro MC, Del Boccio P, Maioli M, Di Stefano A, Cacciatore I
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41493150
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In this work, 17 derivatives were synthesised by combining halogenated and non-halogenated cinnamoyl scaffolds with menthol and tested against a panel of Gram-positive and Gram-negative bacteria. Among the synthesised de...In this work, 17 derivatives were synthesised by combining halogenated and non-halogenated cinnamoyl scaffolds with menthol and tested against a panel of Gram-positive and Gram-negative bacteria. Among the synthesised derivatives, and demonstrated enhanced therapeutic potential. showed the most potent antimicrobial activity (MIC values ranging from 8 to 64 mg/L against ), representing a significant improvement over menthol, with a five-fold reduction in MIC. Additionally, effectively reduced biofilm biomass production by 50% in and by 20% in at sub-MIC concentrations. reduced biomass by up to 40% in at the lowest subMIC concentrations tested (0.06 x MIC). Moreover, showed potential as a wound healing agent promoting fibroblast-mediated repair within just 24 h. Notably, both compounds exhibited no cytotoxic effects. Molecular docking and molecular dynamics simulations confirmed strong binding affinity and high stability of and with the target protein.
Golcienė B, Maciejewska N, Kallingal A
… +3 more, Sapijanskaitė-Banevič B, Stasevych M, Mickevičius V
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41492998
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Imidazole scaffolds are attractive in drug design for bioactivity and synthetic accessibility. We developed S-substituted imidazole-2-thione derivatives, focusing on compound , which showed potent cytotoxicity against lu...Imidazole scaffolds are attractive in drug design for bioactivity and synthetic accessibility. We developed S-substituted imidazole-2-thione derivatives, focusing on compound , which showed potent cytotoxicity against lung, cervical, and colorectal cancer cells with submicromolar IC and selectivity over fibroblasts. Mechanistic analyses revealed G1 arrest, caspase-dependent apoptosis, and p-γH2AX accumulation. Importantly, compound strongly inhibited A-549 cell migration and invasion in both 2D and 3D assays, correlating with downregulation of MMP-2, MMP-9, and hTERT. In vitro enzyme assays further confirmed that compound directly inhibits MMP-9 activity. In vivo, suppressed tumour growth and vasculotropic spread in the CAM model without detectable toxicity. Docking and dynamics simulations confirmed stable binding to MMP-2 and MMP-9 active sites. These results identify compound as a promising anticancer agent with both cytotoxic and anti-metastatic properties, supporting its further preclinical investigation.
Pirone L, Fiorillo B, Del Gatto A
… +7 more, Russo R, Guarracino A, Cassiano C, Zaccaro L, Moraca F, Pedone E, Catalanotti B
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41492994
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UBE2C (also known as UbcH10) is a ubiquitin-conjugating enzyme essential for mitotic progression and a potential therapeutic target in cancer. Here, we report a structure-based design and characterisation of peptides der...UBE2C (also known as UbcH10) is a ubiquitin-conjugating enzyme essential for mitotic progression and a potential therapeutic target in cancer. Here, we report a structure-based design and characterisation of peptides derived from a natural interacting partner (U1) aimed at modulating UBE2C activity. Biophysical and biochemical assays identified peptide as a lead compound, capable of binding UBE2C with micromolar affinity and inhibiting the formation of the UBE2C-Ub thioester complex. Enhanced sampling molecular dynamics simulations revealed that peptide folding landscapes are correlated with activity, with active peptides sampling transient β-sheet conformations compatible with binding. To the best of our knowledge, this is the first report of a peptide inhibitor of UBE2C enzymatic activity.
Ye W, Zheng S, Xie H
… +9 more, Zhou X, Xu J, Luo Q, Huang Y, Li J, Diao J, Luo X, Zhu Q, Liu G
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41492864
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The serine/threonine kinase IKKε is overexpressed or activated in various cancers, making it a promising therapeutic target. Through a large-scale virtual screening of over 12 million compounds, we identified N8 as a nov...The serine/threonine kinase IKKε is overexpressed or activated in various cancers, making it a promising therapeutic target. Through a large-scale virtual screening of over 12 million compounds, we identified N8 as a novel IKKε inhibitor, selected for its favourable docking score and drug-likeness profile. The inhibitory activity of N8 on IKKε was validated in vitro across several cancer cell lines, including HCT116 (colorectal), HepG2 (liver), T24 (bladder), MDA-MB-231 (breast), A549 (lung), and HeLa (cervical). N8 demonstrated significant reductions in cell viability, colony formation, and migration, particularly in HCT116 colorectal cancer cells, where it exhibited superior efficacy compared to established IKKε inhibitors. Mechanistically, N8's anticancer activity appears to be mediated through modulation of autophagy rather than apoptosis.
Fabbian S, Fabi S, Schwarz L
… +7 more, Preto G, Schiavinato C, Salata C, Crocetti L, Battistutta R, Gatto B, Sosic A
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41481484
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The SARS-CoV-2 Main Protease (M), a key enzyme for viral replication, represents a highly attractive target for the development of broad-spectrum anti-coronavirus therapeutics. The organoselenium drug Ebselen has shown p...The SARS-CoV-2 Main Protease (M), a key enzyme for viral replication, represents a highly attractive target for the development of broad-spectrum anti-coronavirus therapeutics. The organoselenium drug Ebselen has shown potent inhibition of M as well as antiviral activity, granting clinical interest as a COVID-19 treatment option. Here we show that Ebselen and selected derivatives with human neutrophil elastase (HNE) inhibition and anti-radical activity are able to bind covalently to the viral enzyme with multiple stoichiometry, exhibiting inhibitory activity towards SARS-CoV-2 M with potencies in the nanomolar range. Employing a mass spectrometry-based approach, we show that, upon binding to the target, Ebselen and its derivatives induce a dose-dependent shift in the dimer-monomer equilibrium, favouring the inactive monomeric state of the viral protease and possibly contributing to the observed inhibition.
Fayed EA, A A Najm M, Oudah KH
… +11 more, Ebrahim MA, Gohar NA, Abu-Elfotuh K, Khedre Mohamed E, Hamdan AME, Albalawi NA, Faisal Alzahrani S, Hamdan AM, Almotairi R, Hafez SM, Ramsis TM
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41481412
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Due to their various pharmacological effects, several substituted sulphur heterocycles containing thiophene have recently attracted a great deal of attention. A novel 2,3-diaryl-2,3,5,6,7,8-hexahydro-4-benzo[4,5]thieno[3...Due to their various pharmacological effects, several substituted sulphur heterocycles containing thiophene have recently attracted a great deal of attention. A novel 2,3-diaryl-2,3,5,6,7,8-hexahydro-4-benzo[4,5]thieno[3,2-][1,3]oxazin-4-one was synthesised starting from cyclohexa[]thiophene. Compounds and showed the greatest gene expression downregulation of BAX by 75.1% and 79.7%, and upregulation of Bcl-2 gene expression by 8.1 folds for each. It also decreased the level of AChE by 70.2 and 75%; respectively. Compounds and significantly increased Wnt3a levels by 5.8 and 6.6 folds, and β-Catenin levels by 10.1 and 10.5 folds, respectively, compared to donepezil. They significantly downregulated 5-GSK3β gene expression by 77.1%, and 78.7%, respectively. Even though all compounds exhibited potent inhibition of AChE, all synthesised compounds, except for compounds and demonstrated higher selectivity towards BChE (SI < 1). ADMET calculations as well as molecular docking have been performed for synthetic compounds.
Chen W, Ye W, Long Y
… +3 more, Zhang Y, Zhou W, Wang W
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41481091
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Cytochrome P4501B1 (CYP1B1), overexpressed in solid tumours but minimally in healthy tissues, is a promising anticancer target linked to chemoresistance. While CYP1B1 inhibitors can restore drug efficacy, most suffer fro...Cytochrome P4501B1 (CYP1B1), overexpressed in solid tumours but minimally in healthy tissues, is a promising anticancer target linked to chemoresistance. While CYP1B1 inhibitors can restore drug efficacy, most suffer from limited scaffold diversity and poor selectivity against other CYPs. We identified 2-(2-phenylethyl) chromones as a novel scaffold for anti-CYP1B1 activity and synthesised 24 derivatives with varied ring A/B substituents and established the SAR. Three compounds (, , ) showed nanomolar anti-CYP1B1 activity and exceptional selectivity (SI > 230). In CYP1B1-overexpressing cells, the water-soluble and non-cytotoxic (solubility > 100 μM) dose-dependently reversed docetaxel resistance, achieving efficacy at 50 μM comparable to 20 μM of the CYP1B1 inhibitor α-naphthoflavone (ANF). Molecular docking revealed similar binding modes for and ANF in CYP1B1's active site. This work hints 2-(2-phenylethyl) chromones as a natural-derived scaffold for promising CYP1B1 inhibitor development.
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41395885
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The study aimed to evaluate the effect of a trypsin inhibitor isolated from tamarind seeds (TTI) as an anti-infective agent. No statistical difference was found in the toxicity test to TTI for locomotion, oviposition, a...The study aimed to evaluate the effect of a trypsin inhibitor isolated from tamarind seeds (TTI) as an anti-infective agent. No statistical difference was found in the toxicity test to TTI for locomotion, oviposition, and progeny parameters. Regarding body size, the tested concentrations of TTI showed a statistical difference and resulted in a greater length of than the control. For bacterial infection analyses, 0.1 mg/mL and 1.0 mg/mL of TTI promoted a survival rate of 16.10% and 30.32%, respectively, higher than the control (8.08%). For the oxidative stress test, all concentrations of TTI presented greater survival than the control at 12h and 18h (p < 0.05). Regarding the bacterial growth curve, no inhibitory activity of TTI was observed in (OP50), nor was antibacterial and antioxidant activity . Therefore, given all the tests, TTI protected under adverse conditions, increasing their survival.
Yang C, Shang Y, Li X
… +3 more, Li J, Li H, Han J
J Enzyme Inhib Med Chem
· 2026 Dec · PMID 41395847
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Poly(ADP-ribose) polymerase (PARP) inhibitors constitute a significant class of targeted anticancer therapies that leverage the principle of synthetic lethality in tumours deficient in homologous recombination (HR) repai...Poly(ADP-ribose) polymerase (PARP) inhibitors constitute a significant class of targeted anticancer therapies that leverage the principle of synthetic lethality in tumours deficient in homologous recombination (HR) repair. Although these agents have shown clinical efficacy in treating HR-deficient tumours, their wider application has been limited by challenges including the emergence of drug resistance, dependency on HR deficiency phenotypes, and related hematological toxicity. To mitigate these limitations, dual-target PARP inhibitors have emerged as a promising therapeutic strategy, simultaneously modulating PARP and synergistic pathways within a single molecular entity. This approach effectively circumvents the pharmacokinetic complexities and cumulative toxicity associated with multi-drug regimens, while simultaneously enhancing therapeutic efficacy through complementary mechanisms. This review highlights recent progress in PARP-based dual inhibitors, focusing on target selection, structure-activity relationships, synergistic antitumor mechanisms, and future research directions. It combines preclinical and clinical insights to guide the development of next-generation PARP dual-target inhibitors with improved efficacy and safety.
Tian Q, Zhang Y, Pan C
… +7 more, Wang L, Qin N, Jiang Z, Li C, Cao Z, Zhu G, Wang P
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41395810
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Isocitrate dehydrogenases (IDHs) regulate the distribution of carbon flux between the TCA cycle and glyoxylate shunt through reversible phosphorylation that influences pathogen virulence. Current studies only indicate th...Isocitrate dehydrogenases (IDHs) regulate the distribution of carbon flux between the TCA cycle and glyoxylate shunt through reversible phosphorylation that influences pathogen virulence. Current studies only indicate that NADP-specific IDHs (NADP-IDHs) can be phosphorylated. Whether NAD-specific IDHs (NAD-IDHs) are susceptible to phosphorylation remains unknown. In this study, two NAD-IDHs and their regulation by phosphorylation from and were characterised for the first time. Ser80 was identified by mass spectrometry as the phosphorylation site in SmIDH, which was functionally validated through site-directed mutagenesis. Acetate induction led to an approximately 78% decrease in the ratio of IDH/ICL specific enzyme activity, consistent with phosphorylation-mediated regulation. By modifying key recognition regions in XsIDH and XsAceK, the phosphorylation efficiency of XsIDH was improved, revealing evolutionary insights. It may enable further investigations for the new antibacterial drug targets in and .
Dong X, Shang B, Li X
… +3 more, Zhang J, Liu Z, Feng B
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41367239
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Sepsis-induced cardiovascular dysfunction (SICD) poses a serious threat to human life. Protein tyrosine phosphatase 1B (PTP1B) displays an essential role in SICD occurrence, so discovering novel inhibitors targeting PTP1...Sepsis-induced cardiovascular dysfunction (SICD) poses a serious threat to human life. Protein tyrosine phosphatase 1B (PTP1B) displays an essential role in SICD occurrence, so discovering novel inhibitors targeting PTP1B is an effective strategy for SICD treatment. In this research, we exploited a novel virtual screening pipeline consisting of both ligand-based and structure-based modules to find novel PTP1B inhibitors, and compound PI-2 with IC = 4.1 ± 0.3 μM was successfully discovered. Enzymatic and cellular thermal shift assay showed PI-2 displayed a moderate PTP1B inhibitory activity and a good selectivity towards both PTP1B and TCPTP. Besides, PI-2 effectively protected Lipopolysaccharide (LPS) induced AC16 injury by reducing cell ROS levels and enhancing mitochondrial membrane potential. Overall, this research not only provides a novel virtual screening strategy for discovering novel PTP1B inhibitors, but also supplies a potential candidate for further optimisation for the treatment of SICD.
Szewczyk-Roszczenko OK, Kotwica-Mojzych K, Roszczenko P
… +6 more, Mojzych M, Rivero-Müller A, Czapla K, Przybyszewska-Podstawka A, Bielawski K, Czarnomysy R
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41342084
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Glioblastoma multiforme (GBM) is a highly aggressive brain tumour with few effective treatment options. This study evaluated two novel triazine-based sulphonamides, MM118 and MM119, for their anticancer effects on GBM ce...Glioblastoma multiforme (GBM) is a highly aggressive brain tumour with few effective treatment options. This study evaluated two novel triazine-based sulphonamides, MM118 and MM119, for their anticancer effects on GBM cells. cell viability assays showed that both compounds were highly potent, killing GBM cells at low-micromolar concentrations. They induced apoptosis in cancer cells, evidenced by Annexin V/PI staining and caspase-3/7 activation. Both the intrinsic and extrinsic apoptosis pathways were engaged, as shown by mitochondrial depolarisation along with caspase-9 and caspase-8 activation. The compounds also increased reactive oxygen species levels, further promoting apoptosis. Notably, MM118 and MM119 triggered pyroptosis - an inflammatory form of cell death - indicated by caspase-1 activation and NF-κB translocation. In a zebrafish xenograft model, both compounds significantly reduced tumour growth. These findings highlight MM118 and MM119 as promising candidates for GBM therapy that may overcome resistance by engaging multiple cell-death pathways.
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41334873
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Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) is crucial in regulating inflammation, apoptosis, and necroptosis. Accumulating evidence highlights RIPK1 as a promising therapeutic target for various human...Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) is crucial in regulating inflammation, apoptosis, and necroptosis. Accumulating evidence highlights RIPK1 as a promising therapeutic target for various human diseases, including neurodegenerative disorders, autoimmune diseases, and cancer. In tumour cells, RIPK1 suppresses immunogenic cell death, promotes an immunosuppressive tumour microenvironment, which facilitates immune evasion, metastatic progression, and therapeutic resistance, contributing to an immunologically cold tumour phenotype. Therefore, targeting RIPK1 represents a promising therapeutic approach to overcome immune checkpoint blockade resistance and convert tumours into an immunologically hot phenotype. In this review, we summarise the biological functions of RIPK1 and elaborate on its roles in cancer progression in terms of the tumour immune microenvironment, tumour metastasis, and chemoresistance. Furthermore, we enumerate several identified RIPK1-targeted inhibitors with potential for cancer therapy. Although RIPK1 has been proposed as a potential anticancer target, there are still great opportunities and challenges that require further investigation.
Xu W, Zhang Y, Xu Q
… +5 more, Zhao H, Gao Q, Zhao X, Jiang H, Wang C
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41324450
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Microtubules, composed of tubulin subunits, represent a critical target in anticancer drug discovery. The design and evaluation of small-molecule inhibitors targeting tubulin polymerisation continue to hold significant p...Microtubules, composed of tubulin subunits, represent a critical target in anticancer drug discovery. The design and evaluation of small-molecule inhibitors targeting tubulin polymerisation continue to hold significant promise for advancing cancer therapeutics. Based on structural insights into tubulin polymerisation inhibitors and tubulin interaction models, a novel series of 3-aryl-4-(3,4,5-trimethoxyphenyl)selenophene derivatives were designed as potential tubulin polymerisation inhibitors. Among the synthesised analogs, compound , featuring a selenophene linker, demonstrated superior antiproliferative activity against Huh7, MCF-7, and SGC-7901 cancer cell lines, with IC values slightly lower than those of combretastatin A-4 (CA-4). Structure-activity relationship studies revealed that electron-donating substituents at the para-position of the B-ring significantly enhanced cytotoxic potency. Mechanistic studies revealed that compound effectively inhibited tubulin polymerisation, disrupted microtubule networks, induced G2/M cell cycle arrest, and triggered apoptosis in cancer cells. These results underscore the potential of incorporating selenophene into the CA-4 scaffold as a promising strategy for developing potent tubulin polymerisation inhibitors, offering new avenues for cancer therapy.
Pham TL, Nguyen VP, Nguyen TTA
… +2 more, Min BS, Kim JA
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41266945
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This study presents the first comprehensive phytochemical analysis of var. leaves, resulting in the isolation of 41 secondary metabolites, including four new compounds: one phenolic () and three bis-iridoid glycosides...This study presents the first comprehensive phytochemical analysis of var. leaves, resulting in the isolation of 41 secondary metabolites, including four new compounds: one phenolic () and three bis-iridoid glycosides (-). The inhibitory activities of these compounds against PTP1B and α-glucosidase were evaluated. Among them, compound exhibited the most potent dual inhibition, with IC values of 8.0 ± 1.1 µM for PTP1B and 3.4 ± 0.2 µM for α-glucosidase. Compounds and showed notable α-glucosidase inhibitory activity, with IC values of 21.9 ± 0.4 µM and 43.8 ± 2.1 µM, respectively. Enzyme kinetics and molecular docking studies revealed their inhibition mechanisms and binding interactions. This study is the first detailed phytochemical investigation of var. and highlights its potential as a natural source of PTP1B and α-glucosidase inhibitors. These findings underscore the plant's promise for developing antidiabetic agents targeting PTP1B and α-glucosidase.
Zheng Y, Qiu H, Zhang K
… +3 more, Ji X, Song M, Deng X
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41263406
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Angiogenesis is pivotal for cancer growth and metastasis, as tumours rely on new blood vessels to progress and spread. Antiangiogenic drugs represent a crucial therapeutic strategy that combats cancer by both obstructing...Angiogenesis is pivotal for cancer growth and metastasis, as tumours rely on new blood vessels to progress and spread. Antiangiogenic drugs represent a crucial therapeutic strategy that combats cancer by both obstructing the development of new blood vessels and disrupting existing tumour-associated vasculature. Recently, significant advancements have been made in antiangiogenic cancer therapies, as evidenced by the extensive literature covered in this review. Numerous novel angiogenesis inhibitors have been reported to exhibit significant efficacy: they not only suppress cancer metastasis and angiogenesis but also induce cancer cell apoptosis via multiple distinct mechanisms. This review comprehensively updates (2014-2025) small molecule angiogenesis inhibitors' design and structure-activity relationship (SAR), integrating latest developments. By systematically analysing the mechanisms of action and distinctive characteristics of these compounds, we aim to offer valuable insights and references to guide the ongoing development of next-generation anti-cancer agents targeting angiogenesis.
Niu X, Zhi J, Feng M
… +5 more, Wang S, Feng X, Jiang X, Chen W, Bai R
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41246973
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The excessive synthesis of melanin leads to skin hyperpigmentation. While tyrosinase activity inhibition has demonstrated efficacy in ameliorating hyperpigmentation, its effectiveness remains limited, and tyrosinase inhi...The excessive synthesis of melanin leads to skin hyperpigmentation. While tyrosinase activity inhibition has demonstrated efficacy in ameliorating hyperpigmentation, its effectiveness remains limited, and tyrosinase inhibitors may induce irritant contact dermatitis. Therefore, there is an imperative need to develop safer and more potent anti-pigmentation agents. Melanin transfer inhibition represents a novel therapeutic strategy for treating hyperpigmentation. This review systematically elucidates the complete process of melanin transfer and its underlying mechanisms. Furthermore, it provides a comprehensive analysis of natural products and small molecule compounds with melanin transfer-inhibiting capabilities, potential compounds that may exhibit anti-pigmentation effects, as well as the binding modes and structure-activity relationships (SARs) of representative compounds. The presented evidence is crucial for identifying and developing novel, highly effective anti-pigmentation medications.
Chen LC, Chang TC, Tseng HJ
… +10 more, Chu JC, Huang YY, Peng HY, Kuo YC, Wu YW, Lin TE, Yen SC, Hsu KC, Huang WJ, Pan SL
J Enzyme Inhib Med Chem
· 2025 Dec · PMID 41246964
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LIMK1 has been demonstrated to be highly correlated with the progression and overall survival rates of colorectal cancer (CRC) patients. In this study, a series of diarylheptanoid scaffold derivatives were intentionally...LIMK1 has been demonstrated to be highly correlated with the progression and overall survival rates of colorectal cancer (CRC) patients. In this study, a series of diarylheptanoid scaffold derivatives were intentionally designed and synthesised to evaluate their potential as LIMK1 inhibitors. Among these compounds, compounds and exhibited LIMK1 inhibitory activity with IC values of 0.94 and 0.57 µM, respectively. We also disclosed the structure-activity relationship of the resulting compounds that exhibited LIMK1 inhibition. Catechol-containing diarylheptanoid was identified as a promising scaffold for LIMK1 inhibitors. Notably, compound demonstrated selectivity in inhibiting the tyrosine kinase-like family and exhibited potent inhibition of CRC cells. Moreover, compound induced an increase in the S phase and a decrease in the G0/G1 phase in a dose-dependent manner, indicating apoptosis induction. These findings establish compound as a lead compound for the further development of anti-CRC agents.