2. Academic Validation
  3. 4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors

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

Affiliation

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.

Figures