Design, Synthesis and Evaluation of Novel 9-substituted Carbazole Derivatives as Potential Anticancer Agents
作者:Nitin Kumar、Devender Pathak
DOI:10.2174/1570180812666150430002118
日期:2015.9.9
energy. Above mentioned compounds were synthesized by starting with carbazole and characterized by FTIR, 1H-NMR, 13C-NMR, MASS spectrometry and elemental analysis. All the synthesized compounds were evaluated for their anticancer activity by SRB assay method against Human Breast Cancer Line (MCF7). All the tested compounds showed moderate to good anticancer activity. Compound 3d and 6c exhibited highest
通过分子对接检查了许多咔唑衍生物对拓扑异构酶的抑制特性,该分子对接由ChemDraw软件设计,然后进行3D优化。两个系列,即2-[(4,5-二氢-2-取代苯基)咪唑-1-基氨基] -1-(9H-咔唑-9-基)乙酮(3a-3e)和2-(9H-咔唑-9发现-yl)-N'-[(4-取代苯基)(哌嗪-1-基)]甲基}乙酰肼(6a-6e)具有最小的结合能。通过以咔唑为原料合成上述化合物,并通过FTIR,1 H-NMR,13表征C-NMR,MASS光谱和元素分析。通过SRB测定法评估所有合成的化合物对人乳腺癌细胞系(MCF7)的抗癌活性。所有测试的化合物均显示出中等至良好的抗癌活性。化合物3d和6c显示出对癌细胞系抑制的最高活性。