吲哚-1,3,4-噻二唑抗癌芳基衍生物的合成及生物学评价

IF 1.8 3区化学 Q3 CHEMISTRY, ORGANIC

Synthetic Communications Pub Date : 2025-01-17 DOI:10.1080/00397911.2024.2431034

Sudhakar Kalagara , Sudhakar Reddy Baddam , Srinivas Ganta , Balaraju Vudari , Sreenivas Enaganti , Anil Damarancha , Laxminarayana Eppakayala

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引用次数: 0

摘要

合成了芳基取代吲哚-1,3,4-噻二唑衍生物（10a-j）文库。采用MTT法研究了新化合物10a-j对MCF-7（乳腺癌）、A549（肺癌）、Colo-205（结肠癌）和A2780（卵巢癌）4种人癌细胞的体外抗癌作用。将所得IC50值与以依托泊苷为阳性对照进行比较。化合物的IC50值为11.6±8.54µM, 3.34±0.152µM。在合成的化合物中，化合物10a、10b和10c表现出比阳性对照更高的细胞毒活性。

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Synthesis and biological evaluation of aryl derivatives of indole-1,3,4-thiadiazole as anticancer agents

A library of aryl substituted indole-1,3,4-thiadiazole derivatives (10a–j) is synthesized. The in vitro anticancer properties of newly developed compounds 10a–j were investigated against four human cancer cell lines like MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer) and A2780 (ovarian cancer) by employing of MTT assay. The obtained IC₅₀ value was compared with etoposide which was used as positive control. The promising IC₅₀ values of compounds 11.6 ± 8.54 µM, 3.34 ± 0.152 µM. Among the synthesized compounds, three compounds 10a, 10b and 10c displayed more cytotoxic activity than positive control.

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来源期刊

Synthetic Communications 化学-有机化学

CiteScore

4.40

自引率

4.80%

发文量

156

审稿时长

4.3 months

期刊介绍： Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.