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噻唑烷酮连接的 1,2,3-三唑类化合物,以(R)-香芹酮为新型潜在抗癌药物。

Thiazolidinone-linked-1,2,3-triazoles with (R)-Carvone as new potential anticancer agents.

机构信息

Laboratory of Organic & Physical Chemistry, Applied Bioorganic Chemistry Team, Faculty of Sciences, Iboun Zohr University, Agadir, Morocco.

Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam bin Abdulaziz University, Al-Kharj, 11942, Saudi Arabia.

出版信息

Future Med Chem. 2024;16(14):1449-1464. doi: 10.1080/17568919.2024.2351287. Epub 2024 May 30.

Abstract

This study explores the cytotoxic and apoptotic effects of novel thiazolidinone-1,2,3-triazole hybrids on HT-1080, A-549, and MDA-MB-231 cancer cell lines. The synthesized compounds underwent comprehensive characterization (NMR and HRMS) to confirm their structures and purity. Subsequent anticancer activity screening across diverse cancer cell lines revealed promising antitumor potential notably, compounds and . Mechanistic investigations unveiled that compound triggers apoptosis through the caspase-3/7 pathway. In terms of studies, the compound was identified as a potent inhibitor of caspase-3 and caspase-7. The present study underscores the therapeutic potential of thiazolidinone-1,2,3-triazole hybrids against certain cancer cells. These findings highlight a promising avenue for the development of cancer treatment strategies utilizing these (R)-Carvone-based derivatives.

摘要

本研究探讨了新型噻唑烷酮-1,2,3-三唑杂合体对 HT-1080、A-549 和 MDA-MB-231 癌细胞系的细胞毒性和细胞凋亡作用。合成的化合物经过全面表征(NMR 和 HRMS)以确认其结构和纯度。随后对不同癌细胞系的抗癌活性筛选显示出有希望的抗肿瘤潜力,特别是化合物 和 。机制研究表明,化合物 通过 caspase-3/7 途径引发细胞凋亡。在 研究中,化合物 被鉴定为 caspase-3 和 caspase-7 的有效抑制剂。本研究强调了噻唑烷酮-1,2,3-三唑杂合体对某些癌细胞的治疗潜力。这些发现为利用这些(R)-香芹酮衍生的化合物开发癌症治疗策略提供了一个有前途的途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e45e/11352694/882691eca000/IFMC_A_2351287_UF0001_C.jpg

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