Synthesis and biological evaluation of curcumin inspired indole analogues as tubulin polymerization inhibitors

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• 作者：P.V. Sri Ramya^a ; Srinivas Angapelly^a ; Lalita Guntuku^b ; Chander Singh Digwal^a ; Bathini Nagendra Babu^a ; V.G.M. Naidu^b ; ; Ahmed Kamal^a ; ^{ahmedkamal@iict.res.in}
• 关键词：Curcumin mimics ; Indole ; Cytotoxic ; Apoptosis ; Cell cycle ; Claisen-Schmidt condensation
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：100-114
• 全文大小：2924 K
• 卷排序：127

文摘

Novel curcumin inspired indole analogues were synthesized. Anticancer activity was tested on selected eight human cancer cell lines and one normal cell line. The target compounds 11c and 11f effectively inhibited polymerization of tubulin in a cell-free assay. 11c and 11f induced apoptosis and collapse of DΨm in PC3 cells. 11c arrested PC3 cells in G2/M phase of cell cycle.