Emerging therapeutic strategies in cancer therapy by HDAC inhibition as the chemotherapeutic potent and epigenetic regulator

Medical Oncology, Год журнала: 2024, Номер 41(4)

Опубликована: Март 5, 2024

Язык: Английский

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Oxadiazole derivatives: Histone deacetylase inhibitors in anticancer therapy and drug discovery

European Journal of Medicinal Chemistry Reports, Год журнала: 2022, Номер 5, С. 100058 - 100058

Опубликована: Май 23, 2022

Heterocycles are being playing an important role in cancer treatment for years. Currently, a number of anticancer agents available on market, but concerns such as less effectiveness, drug resistance, adverse effects, and non-selectivity create urgent need the development newer highly potent with fewer side effects. Among heterocycles, oxadiazole is great interest recent era due to their potential activity. Structurally, five-member heterocyclic ring that contains one oxygen two nitrogen heteroatom. The mechanism cell suppression involve inhibition different growth factors enzymes including histone deacetylase (HDAC), thymidylate synthase (TS), vascular endothelial factor (VEGF), glycogen kinase-3 (GSK), epidermal (EGF), etc. HDAC considered target therapy discovery. inhibitors act by promoting acetylation histones, regulate cause death pathways, like apoptosis, differentiation, cycle arrest DNA repair, up-regulation or reactivation silenced tumor suppressors, down regulation factors. Recently, five drugs namely Vorinostat (SAHA), Romidepsin (FK-228), Belinostat (PXD-101), Panobinostat (LBH-589), Chidamide have been granted US/Chinese FDA several queue clinical trials. focused area this review summarize current status, chemistry, structure activity relationship, action, therapeutic various derivatives novel inhibiting enzymes. Finally, we highlighted future prospects agents.

Язык: Английский

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Synthesis, Anticancer Activity and Computational Docking Techniques of Some Novel Derivatives Based on Indole Bearing Oxadiazole–Triazole Moieties

Russian Journal of Bioorganic Chemistry, Год журнала: 2023, Номер 49(3), С. 629 - 644

Опубликована: Май 11, 2023

Язык: Английский

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Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 261, С. 115800 - 115800

Опубликована: Сен. 9, 2023

Язык: Английский

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Design, synthesis and biological evaluation of novel substituted indazole-1,2,3-triazolyl-1,3,4-oxadiazoles: Antimicrobial activity evaluation and docking study

Results in Chemistry, Год журнала: 2022, Номер 4, С. 100605 - 100605

Опубликована: Янв. 1, 2022

A novel series of dual 1,2,3–triazole and 1,3,4–oxadiazole heterocyclic compounds linked to indazole were designed efficiently synthesized using 3-bromo-1H-indazole as potential antimicrobial agents. All the characterized by their proton, carbon nuclear magnetic resonance, infrared, mass spectral data, elemental analysis. The final 9a–m evaluated in vitro activity against Gram–negative microorganism E. coli, Gram–positive microorganisms B. subtilis, S. pneumoniae, aureus antifungal strains A. fumigates, C. albicans. From biological screening, we surprised find that most have significant inhibitory particular heterocycles 9b, 9c, 9h, 9i, 9j showed outstanding antibacterial bacteria pneumoniae with MICs 5.4 ± 0.02, 5.8 0.03, 8.0 0.04, 4.0 7.8 0.01 µg/mL respectively, when compared ampicillin [MIC = 9.1 µg/mL]. Final prepared scaffolds 9h acquiring highest drug scores ΔG –7.78, –8.34 Kcal/mol amino acids residues Arg171 (O…H: 1.934), Lys20 (N…H: 1.951), Arg265 2.080), ArgA:171 (2.740), ArgA:265 (1.874), TyrA:248 (1.973), Ser19 (H…O: 2.048), Tyr248 1.570), 1.976), Arg46 1.059) ArgA:45 (O…H, 2.94 Å) respectively.

Язык: Английский

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Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 262, С. 115879 - 115879

Опубликована: Окт. 18, 2023

Язык: Английский

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Exploring β-carboline hybrids and their derivatives: A review on synthesis and anticancer efficiency

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 288, С. 117412 - 117412

Опубликована: Фев. 18, 2025

Язык: Английский

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Design and Synthesis of Riluzole-Ciprofloxacin Hybrids as Highly Selective Mst3 Inhibitors for Cancer Treatment

Опубликована: Янв. 1, 2025

Язык: Английский

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Vorinostat, a potential hormetin, extends lifespan and enhances stress resistance via the SKN-1 pathway in Caenorhabditis elegans

Biogerontology, Год журнала: 2025, Номер 26(3)

Опубликована: Апрель 25, 2025

Язык: Английский

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Synthesis, Anticancer Activity and Molecular Docking Studies of Novel N-Mannich Bases of 1,3,4-Oxadiazole Based on 4,6-Dimethylpyridine Scaffold

International Journal of Molecular Sciences, Год журнала: 2022, Номер 23(19), С. 11173 - 11173

Опубликована: Сен. 22, 2022

Cancer is one of the greatest challenges in modern medicine today. Difficult and long-term treatment, many side effects drugs used growing resistance to treatment neoplastic cells necessitate new approaches therapy. A very promising targeted therapy based on direct impact only cancer cells. As a continuation our research biologically active molecules, we report herein design, synthesis anticancer evaluation series N-Mannich-base-type hybrid compounds containing morfoline or different substituted piperazines moieties, 1,3,4-oxadiazole ring 4,6-dimethylpyridine core. All were tested for their potential cytotoxicity against five human cell lines, A375, C32, SNB-19, MCF-7/WT MCF-7/DX. Two N-Mannich bases (compounds 5 6) further evaluated growth inhibition melanoma (A375 C32), normal (HaCaT) lines using clonogenic assay population doubling time test. The apoptosis was determined with neutral version comet assay. confocal microscopy method enabled visualization F-actin reorganization. obtained results demonstrated that 6 have cytotoxic proapoptotic are capable inducing depolarization dose-dependent manner. Moreover, computational chemistry approaches, molecular docking electrostatic employed study non-covalent interactions investigated four receptors. It found all examined molecules exhibit similar binding affinity respect chosen reference drugs.

Язык: Английский

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