Synthesis and biological evaluation of amide derivatives of 1,2,4-thiadiazole-thiazole-pyridine as anticancer agents

IF 2.218 Q2 Chemistry Chemical Data Collections Pub Date : 2023-12-15 DOI:10.1016/j.cdc.2023.101108

Somaiah Nalla , Y. Pavani , Ravi kumar Gollapudi , Sumalatha Poodari , Subbarao Mannam

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Abstract

A new series of amide derivatives (10a–j) were designed and synthesized and their structures were confirmed by analytical data. Further, all these derivatives (10a–j) were examined for in vitro antitumor activity against four human cancer cell lines like MCF-7 (breast), A549 (lung), Col-205 (colon) and A2780 (ovarian) by using of the MTT assay. All the derivatives (10a–j) were exhibited remarkable anticancer effects on four cell lines as compared with etoposide used as a positive control. The IC₅₀ values range of tested compounds from 0.11 ± 0.051 µM to 7.42 ± 5.89 µM; whereas, positive control showed IC₅₀ values ranges from 0.17 ± 0.034 µM to 3.34 ± 0.152 µM, respectively. Among these derivatives, four compounds 10a, 10b, 10c & 10d demonstrated more potent activities than the positive control.

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作为抗癌剂的 1,2,4-噻二唑-噻唑-吡啶酰胺衍生物的合成与生物学评价

我们设计并合成了一系列新的酰胺衍生物（10a-j），并通过分析数据确认了它们的结构。此外，还利用 MTT 试验检测了所有这些衍生物（10a-j）对四种人类癌细胞株，如 MCF-7（乳腺癌）、A549（肺癌）、Col-205（结肠癌）和 A2780（卵巢癌）的体外抗肿瘤活性。与作为阳性对照的依托泊苷相比，所有衍生物（10a-j）对四种细胞系都表现出了显著的抗癌效果。测试化合物的 IC50 值范围为 0.11±0.051 µM 至 7.42±5.89 µM；而阳性对照的 IC50 值范围分别为 0.17 ± 0.034 µM 至 3.34 ± 0.152 µM。在这些衍生物中，4 个化合物 10a、10b、10c&10d 比阳性对照显示出更强的活性。

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来源期刊

Chemical Data Collections Chemistry-Chemistry (all)

CiteScore

6.10

自引率

0.00%

发文量

169

审稿时长

24 days

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