Synthesis and Evaluation of Anticancer Activity of Indazole Derivatives
Synthesis and Evaluation of Anticancer Activity of Indazole Derivatives
复制标题
DOI：
10.1134/s1070363218110233
复制
发表时间：
2018-11-01
影响因子：
0.9
通讯作者：
Rao, B. Venteswar
中科院分区：
文献类型：
--
作者：
Reddy, G. Sandeep;Mohanty, S.;Rao, B. Venteswar
合成了一系列新型吲唑13a-13j衍生物。它们的结构通过 H-1 和 C-13 NMR 以及质谱分析得到证实。使用考布他汀-A4 作为阳性对照，测试了这些化合物对四种人类癌细胞系的抗癌活性，包括 A549（肺）、MCF7（乳腺癌）、A375（黑色素瘤）和 HT-29（结肠）。大多数合成的化合物对上述细胞系表现出有效的活性。此处，目标化合物的 IC50 值范围为 0.010 +/- 0.0042 至 12.8 +/- 3.77 M，对照药物的范围为 0.11 +/- 0.02 至 0.93 +/- 0.034 M。确定化合物 13a、13b、13e、13g、13h 和 13j 比阳性对照更有效。
A novel series of indazole 13a-13j derivatives has been synthesized. Their structures are confirmed by H-1 and C-13 NMR, and mass spectral analysis. The compounds are tested for their anticancer activity against four human cancer cell lines including A549 (Lung), MCF7 (Breast), A375 (Melanoma), and HT-29 (Colon), using combretastatin-A4 as a positive control. Most of the synthesized compounds demonstrate potent activity against the above cell lines. Here IC50 values of target compounds range from 0.010 +/- 0.0042 to 12.8 +/- 3.77 M and the control drug from 0.11 +/- 0.02 to 0.93 +/- 0.034 M. The compounds 13a, 13b, 13e, 13g, 13h, and 13j are determined to be more potent than the positive control.