Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures
Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures
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仅具有氧杂环丁烷D环和侧链结构的紫杉醇模拟物的设计、合成和生物学评价
DOI：
10.1016/j.fitote.2013.10.015
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发表时间：
2014-01-01
期刊：
影响因子：
3.4
通讯作者：
Wang, Dan
中科院分区：
文献类型：
--
作者：
Chen, Xing-Xiu;Gao, Feng;Wang, Dan
在分析紫杉醇构效关系的基础上，设计并合成了两个仅含氧杂环丁烷D环和C-13侧链的螺环紫杉醇模拟物。体外微管稳定和抗增殖试验表明，模拟物的活性比紫杉醇弱，但这仍然代表了具有显著抗肿瘤生物活性的简化紫杉醇类似物的第一个例子。(C)2013爱思唯尔有限公司版权所有。
Two Spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than paclitaxel, but which still represented the first example of simplified paclitaxel analogues with significant anti-tumor biological activity. (C) 2013 Elsevier B.V. All rights reserved.