2. Academic Validation
  3. Semi-synthetic aristolactams--inhibitors of CDK2 enzyme

Semi-synthetic aristolactams--inhibitors of CDK2 enzyme

  • Bioorg Med Chem Lett. 2010 Feb 15;20(4):1384-7. doi: 10.1016/j.bmcl.2010.01.007.
Vinod R Hegde 1,  Scott Borges,  Haiyan Pu,  Mahesh Patel,  Vincent P Gullo,  Bonnie Wu,  Paul Kirschmeier,  Michael J Williams,  Vincent Madison,  Thierry Fischmann,  Tze-Ming Chan
Affiliations

Affiliation

  • 1 Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
PMID: 20097066 DOI: 10.1016/j.bmcl.2010.01.007
Abstract

Several analogs of aristolochic acids were isolated and derivatized into their lactam derivatives to study their inhibition in CDK2 assay. The study helped to derive some conclusions about the structure-activity relation around the phenanthrin moiety. Semi-synthetic aristolactam 21 showed good activity with inhibition IC50 of 35 nM in CDK2 assay. The activity of this compound was comparable to some of the most potent synthetic compounds reported in the literature.

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