Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents

…, C Sheng, Z Lv, G Dong, T Wang, J Liu…

文献索引：Chen, Huan; Li, Yongmei; Sheng, Chunquan; Lv, Zhiliang; Dong, Guoqiang; Wang, Tiantian; Liu, Jia; Zhang, Mingfeng; Li, Lingzhen; Zhang, Tao; Geng, Dongping; Niu, Chunjuan; Li, Ke Journal of Medicinal Chemistry, 2013 , vol. 56, # 3 p. 685 - 699

全文：HTML全文

被引用次数: 18

摘要

A series of novel cyclopropylamide analogues of combretastatin-A4 (CA-4) were designed and synthesized. Most of them had significant in vitro antiproliferative activities, particularly for compounds 7i4, 7c4, 8a4, and 8c4. Moreover, compound 8c4 was also equally potent against paclitaxel resistant cancer cells. Interestingly, the novel cyclopropylamide analogues had different binding mechanisms from CA-4. Instead of inhibiting tubulin polymerization, ...