Synthesis and Anticancer Activity of 3-(Substituted Aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole Derivatives

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• 作者：Xiao-Ping Zhan ; Lan Lan ; Shuai Wang ; Kai Zhao ; Yu-Xuan Xin ; Qi Qi ; Yao-Lin Wang and Zhen-Min Mao
• 刊名：Chemistry & Biodiversity
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：14
• 期：2
• 全文大小：264K
• ISSN：1612-1880

文摘

A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized compounds, compound 3f was the most potent compound against A375, CT-26, HeLa, MGC80-3, NCI-H460 and SGC-7901 cells (IC₅₀ = 8.2 – 31.7 μm); 3g, 3n and 3a were the most potent compounds against CHO (IC₅₀ = 8.2 μm), HCT-15 (IC₅₀ = 21 μm) and MCF-7 cells (IC₅₀ = 18.7 μm), respectively. Importantly, all the target compounds showed no cytotoxicity towards the normal tissue cell (IC₅₀ > 100 μm). Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.