4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors

  • Bioorg Med Chem Lett. 2006 Jun 15;16(12):3121-4. doi: 10.1016/j.bmcl.2006.03.059.
Zhi-Jie Ni  1 ,  Paul Barsanti ,  Nathan Brammeier ,  Anthony Diebes ,  Daniel J Poon ,  Simon Ng ,  Sabina Pecchi ,  Keith Pfister ,  Paul A Renhowe ,  Savithri Ramurthy ,  Allan S Wagman ,  Dirksen E Bussiere ,  Vincent Le ,  Yasheen Zhou ,  Johanna M Jansen ,  Sylvia Ma ,  Thomas G Gesner
Affiliations
  • 1. Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA. [email protected]
PMID: 16603354 DOI: 10.1016/j.bmcl.2006.03.059
Abstract

CHK-1 is one of the key Enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and assayed for their ability to inhibit CHK-1. These compounds are potent cell permeable CHK-1 inhibitors and showed synergistic effect with a DNA-damaging agent, camptothecin.