Novel tubulin interacting agents

CHED 981

Kyle Chastain, mbearcat60@hotmail.com and Maralea Gourley, gourlem@hsu.edu. Department of Chemistry, Henderson State University, Reynolds Rm 315, Arkadelplhia, AR 71999
A number of antimitotic agents interfere with tubulin stabilization. Colchicine is one such agent that prevents tubulin to polymerize. Agents that inhibit the binding of colchicine bind in a common site referred to as the colchicine domain. These antimitoic agents include an array of diverse compounds and their derivatives.

Using molecular modeling a pharmacophore was generated to include all the diverse subsets of colchicine binding drugs. This model allowed us to find novel commercially available agents to evaluate their antimitoic properties.

Microtubule polymerization assays were performed with these agents to determine the concentration that inhibited tubulin polymerization by 50% (IC50).