Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 274, С. 116535 - 116535

Опубликована: Май 31, 2024

Язык: Английский

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Targeting DNA repair mechanisms: Spirobenzoxazinone and salicylamide derivatives as novel candidates for PARP-1 inhibition in cancer therapy

Bioorganic & Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 118173 - 118173

Опубликована: Март 1, 2025

Язык: Английский

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Targeting selective inhibitors of PARPs in drug discovery and development

Medicinal Chemistry Research, Год журнала: 2024, Номер 33(10), С. 1734 - 1756

Опубликована: Июль 28, 2024

Язык: Английский

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Computational approach: 3D-QSAR, molecular docking, ADMET, molecular dynamics simulation investigations, and retrosynthesis of some curcumin analogues as PARP-1 inhibitors targeting colon cancer

New Journal of Chemistry, Год журнала: 2023, Номер 47(45), С. 20987 - 21009

Опубликована: Янв. 1, 2023

As cancer is the second-leading cause of death globally, this study strives to find efficient medications for colon that minimal side effects.

Язык: Английский

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Synthesis, docking study, and antitumor evaluation of benzamides and oxadiazole derivatives of 3‐phenoxybenzoic acid as VEGFR‐2 inhibitors

Drug Development Research, Год журнала: 2024, Номер 85(3)

Опубликована: Апрель 20, 2024

Abstract Current chemotherapeutic agents have several limitations, including lack of selectivity, the development undesirable side effects, and chemoresistance. As a result, there is an unmet need for novel small molecules with minimal effects ability to specifically target tumor cells. A new series 3‐phenoxybenzoic acid derivatives, 1,3,4‐oxadiazole derivatives ( 4a–d ) benzamides 5a–e were synthesized; their chemical structures confirmed by Fourier‐transform infrared spectroscopy, 1 H nuclear magnetic resonance (NMR), 13 C NMR, mass spectra; various physicochemical properties determined. The antiproliferative activities evaluated means 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. Three compounds 4b , 4c 4d exhibited cytotoxicity against two three cell lines tested, five 3 4a 5a 5b 5e toxic one line, while 5c 5d not cytotoxic any tested in current study. Based on docking scores, MTT assay findings, vascular endothelial growth factor receptor 2 (VEGFR‐2) kinase activity data, Compound was selected further biological investigation. Flow cytometry used determine mode death (apoptosis vs. necrosis) effect cycle progression. arrested HepG2 hepatocellular carcinoma cells G2/M phase activated both intrinsic extrinsic apoptosis pathways. In conclusion, has shown promising results future research as potent VEGFR‐2 tyrosine inhibitor.

Язык: Английский

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An update on small molecule compounds targeting synthetic lethality for cancer therapy

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 278, С. 116804 - 116804

Опубликована: Сен. 2, 2024

Язык: Английский

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Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 277, С. 116726 - 116726

Опубликована: Июль 31, 2024

Язык: Английский

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The recent advance and prospect of poly(ADP‐ribose) polymerase inhibitors for the treatment of cancer

Medicinal Research Reviews, Год журнала: 2024, Номер 45(1), С. 214 - 273

Опубликована: Авг. 24, 2024

Chemotherapies are commonly used in cancer therapy, their applications limited to low specificity, severe adverse reactions, and long-term medication-induced drug resistance. Poly(ADP-ribose) polymerase (PARP) inhibitors a novel class of antitumor drugs developed solve these intractable problems based on the mechanism DNA damage repair, which have been widely applied treatment ovarian cancer, breast other cancers through inducing synthetic lethal effect trapping PARP-DNA complex BRCA gene mutated cells. In recent years, PARP combination with various first-line chemotherapy drugs, targeted immune checkpoint expand scope clinical application. However, intricate mechanisms underlying resistance inhibitors, including restoration homologous recombination, stabilization replication forks, overexpression efflux protein, epigenetic modifications pose great challenges desirability development inhibitors. this review, we will focus mechanism, structure-activity relationship, multidrug associated representative Furthermore, aim provide insights into prospects emerging trends offer guidance for application inspiration degraders.

Язык: Английский

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Discovery of 3-(2-aminobenzo[d]thiazol-5-yl) benzamide derivatives as potent anticancer agents via ROR1 inhibition

Bioorganic & Medicinal Chemistry, Год журнала: 2024, Номер 117, С. 118011 - 118011

Опубликована: Ноя. 20, 2024

Язык: Английский

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