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Synthesis and Activity of Epothilone D.
Current Drug Targets ( IF 3.0 ) Pub Date : 2018-08-04 , DOI: 10.2174/1389450119666180803122118
Hao Cheng 1 , Gangliang Huang 1
Affiliation  

Epothilones are a class of macrolide compounds. Their activities of tubulin polymerization and microtubule depolymerization inhibition like paclitaxel make them a new generation of antimitotic drugs. The mechanism of action is similar to that of paclitaxel, which can bind to tubulin and cause cancer cells to fail to undergo mitosis, thereby causing apoptosis in cancer cells. Epothilone is superior to paclitaxel in anti-tumor spectrum, anti-tumor activity, safety, water solubility and synthetic methods. It is expected to develop into a more effective anti-tumor drug than paclitaxel. Herein, the synthesis methods and activity of epothilone D were summarized and analyzed.

中文翻译:

埃坡霉素D的合成与活性

上环酮是一类大环内酯化合物。它们的微管蛋白聚合和微管解聚抑制活性(如紫杉醇)使其成为新一代的抗有丝分裂药物。作用机理与紫杉醇相似,紫杉醇可与微管蛋白结合并导致癌细胞无法进行有丝分裂,从而导致癌细胞凋亡。埃博霉素在抗肿瘤谱,抗肿瘤活性,安全性,水溶性和合成方法方面均优于紫杉醇。有望发展成为比紫杉醇更有效的抗肿瘤药。在此,总结并分析了埃坡霉素D的合成方法和活性。
更新日期:2019-11-01
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