Related Experiment Videos
Synthesis and biological evaluation of novel macrocyclic paclitaxel analogues
B B Metaferia1, J Hoch, T E Glass
1Departments of Chemistry, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA.
Organic Letters
|August 3, 2001
Abstract:
[reaction: see text] 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.