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Synthesis and in vitro anti-proliferative capabilities of steroidal thiazole and indole derivatives
Journal of Saudi Chemical Society ( IF 5.6 ) Pub Date : 2019-05-16 , DOI: 10.1016/j.jscs.2019.05.001
Fariha Shamim , Kanwal , Firdos Alam Khan , Muhammad Taha , Khalid Mohammed Khan , Arshia

Derivatives (115) of steroidal and indole class were synthesized using different strategies. These compounds were characterized by 1H NMR spectroscopy and EI-MS, respectively. The synthetic derivatives were examined for their cytotoxic effects on human adenocarcinoma cells (HCT-116) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and morphometric analysis. The cytotoxic effects of all the compounds were observed after 48 h treatment and it was found that out of fifteen, four compounds 1, 2, 3, and 14 showed inhibitory action on the cancer cells. We have calculated the IC50 values for compounds 1, 2, 3, and 14 which were 22.50 µg/mL, 55.65 µg/mL, 21.35 µg/mL and 58.50 µg/mL, respectively. The compounds 3 (IC50 = 21.35 µg/mL) and 1 (IC50 = 22.50 µg/mL) showed highest inhibitory activities as compared to compounds 2 (IC50 = 55.65 µg/mL) and 14 (IC50 = 58.50 µg/mL). These results suggested that steroidal thiazole and indole derivatives are potent lead molecules having strong anti-cancer proliferative capabilities.



中文翻译:

甾族噻唑和吲哚衍生物的合成及其体外抗增殖能力

类固醇和吲哚类的衍生物(115)是使用不同的策略合成的。这些化合物分别通过1 H NMR光谱和EI-MS进行表征。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物(MTT)测定法和形态计量分析检查了合成衍生物对人腺癌细胞(HCT-116)的细胞毒性作用。48小时处理后,观察所有的化合物的细胞毒性作用,并且发现了这一点的15,四种化合物123,和14显示出对癌细胞的抑制作用。我们已经计算了化合物的IC 50123,和14,其分别为22.50微克/毫升,分别55.65微克/毫升,21.35微克/毫升和58.50微克/毫升。 与化合物2(IC 50  = 55.65 µg / mL)和14(IC 50  = 58.50μg / mL)相比,化合物3(IC 50  = 21.35μg/ mL)和1(IC 50 = 22.50μg/ mL)表现出最高的抑制活性。毫升)。这些结果表明,甾族噻唑和吲哚衍生物是具有强的抗癌增殖能力的有效的先导分子。

更新日期:2019-05-16
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