Synthesis, antitumor evaluation, and molecular docking studies of indole–indazolyl hydrazide–hydrazone derivatives
Synthesis, antitumor evaluation, and molecular docking studies of indole–indazolyl hydrazide–hydrazone derivatives
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DOI：
10.1007/s00706-016-1750-6
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发表时间：
2017-02
期刊：
影响因子：
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通讯作者：
R. Sreenivasulu;P. Sujitha;S. S. Jadav-S.;M. Ahsan;C. Kumar;R. Raju
中科院分区：
文献类型：
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作者：
R. Sreenivasulu;P. Sujitha;S. S. Jadav-S.;M. Ahsan;C. Kumar;R. Raju
摘要：设计并合成了10个新型的吲哚和茚唑基团的腙类化合物。所有合成的化合物对四种人类癌细胞系（HeLa、MDA-MB-231、MCF-7和A549）的细胞毒性进行了评估。其中三种合成的化合物在一些被测试的细胞系上表现出很好的细胞毒性，ic50值在1.93到25.6µM之间。此外，一种化合物被确定为有前景的药物先导物，与标准药物阿霉素（ic50值0.98µM）相比，该化合物对MCF-7乳腺癌细胞系显示出良好的细胞毒性，ic50值为1.93µM。而这些新化合物对正常人胚胎肾细胞株HEK-293均无细胞毒性。图形抽象
AbstractA series of ten novel hydrazide–hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promising cytotoxicity specifically on some of the tested cell lines withIC50values ranging between 1.93 and 25.6 µM. Further, one compound was identified as a promising drug lead which showed promising cytotoxicity withIC50value of 1.93 µM towards MCF-7 breast cancer cell line as compared to the standard drug doxorubicin (IC50value 0.98 µM). While, all these new compounds showed no cytotoxicity on the normal human embryonic kidney cell line, HEK-293.Graphical abstract