Issue 2, 2013

Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site

Abstract

The synthesis, biological evaluation and molecular modeling of a series of pyrrole compounds related to 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid that evaluates and optimizes C-4 substituents are reported. The key factor for microtubule depolymerization activity appears to be the presence of an appropriately positioned acceptor for Cys241β in the otherwise hydrophobic subpocket A.

Graphical abstract: Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site

Supplementary files

Article information

Article type
Concise Article
Submitted
24 Oct 2012
Accepted
10 Dec 2012
First published
17 Dec 2012

Med. Chem. Commun., 2013,4, 417-421

Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site

C. Da, N. Telang, K. Hall, E. Kluball, P. Barelli, K. Finzel, X. Jia, J. T. Gupton, S. L. Mooberry and G. E. Kellogg, Med. Chem. Commun., 2013, 4, 417 DOI: 10.1039/C2MD20320K

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