Synthesis and biological evaluation of novel macrocyclic paclitaxel analogues

被引：42

作者：

Metaferia, BB

Hoch, J

Glass, TE

Bane, SL

Chatterjee, SK

Snyder, JP ^{[1
]}

Lakdawala, A

Cornett, B

Kingston, DGI

机构：

[1] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA

[2] SUNY Binghamton, Dept Chem, Binghamton, NY 13902 USA

[3] Emory Univ, Dept Chem, Atlanta, GA 30322 USA

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 16期

关键词：

D O I：

10.1021/ol016124d

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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.

引用

页码：2461 / 2464

页数：4

共 29 条

[1]

[Anonymous], 1995, Taxol: Sci. Appl

[2] Synthesis and NMR-driven conformational analysis of taxol analogues conformationally constrained on the C13 side chain [J].