Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency

  • ACS Med Chem Lett. 2012 Jan 12;3(1):35-38. doi: 10.1021/ml200195s.
Wan Seok Yang  1 ,  Kenichi Shimada ,  Darnelle Delva ,  Milesh Patel ,  Egberamwen Ode ,  Rachid Skouta ,  Brent R Stockwell
Affiliations
  • 1. Department of Biological Sciences, Department of Chemistry, and Howard Hughes Medical Institute, Columbia University , Northwest Corner Building, 12th Floor, 550 West 120th Street, MC 4846, New York, New York 10027, United States.
PMID: 22247791 DOI: 10.1021/ml200195s
Abstract

We analyzed more than 1 million small molecules with the goal of finding simple synthetic compounds that potently inhibit Cancer cell growth. We identified three such compounds with unknown mechanisms of action. Subsequent studies revealed that all three of these small molecules target microtubules. These three scaffolds can serve as templates for developing new microtubule-targeted agents, overcoming the limits of existing microtubule-inhibiting drugs derived from complex natural products.

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