Synthesis and biological evaluation of novel macrocyclic paclitaxel analogues.
ORGANIC LETTERS(2001)
摘要
[GRAPHICS] This work describes the synthesis of two novel macrocyclic taxoid constructs by ring-closing olefin metathesis (RCM) and their biological evaluation. Computational studies examine conformational profiles of 1 and 2 for their fit to the beta -tubulin binding site determined by electron crystallography. The results support the hypothesis that paclitaxel binds to microtubules in a "T" conformation.
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关键词
metathesis reactions,terpenes
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