摘要
Epothilone是一类大环内酯类化合物。它们的微管蛋白聚合活性和紫杉醇对微管解聚的抑制作用使其成为新一代抗核药物。其作用机制与紫杉醇相似,可与微管蛋白结合,使癌细胞不能进行有丝分裂,从而导致癌细胞凋亡。在抗肿瘤光谱、抗肿瘤活性、安全性、水溶性和合成方法等方面均优于紫杉醇。它有望发展成为比紫杉醇更有效的抗肿瘤药物。本文对环氧酮D的合成方法和活性进行了综述和分析。
关键词: 环氧酮D,合成,活性,微管,解聚,紫杉醇。
图形摘要
Current Drug Targets
Title:Synthesis and Activity of Epothilone D
Volume: 19 Issue: 15
关键词: 环氧酮D,合成,活性,微管,解聚,紫杉醇。
摘要: 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.
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Cite this article as:
Synthesis and Activity of Epothilone D, Current Drug Targets 2018; 19 (15) . https://dx.doi.org/10.2174/1389450119666180803122118
DOI https://dx.doi.org/10.2174/1389450119666180803122118 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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