Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases

Kelly Frazier; Elisa Jazan; Christopher M McBride; Sabina Pecchi; Paul A Renhowe; Cynthia M Shafer; Clarke Taylor; Dirksen Bussiere; Molly Min He; Johanna M Jansen; Gena Lapointe; Sylvia Ma; Jayesh Vora; Marion Wiesmann

doi:10.1016/j.bmcl.2006.01.020

Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2247-51. doi: 10.1016/j.bmcl.2006.01.020. Epub 2006 Jan 30.

Authors

Kelly Frazier¹, Elisa Jazan, Christopher M McBride, Sabina Pecchi, Paul A Renhowe, Cynthia M Shafer, Clarke Taylor, Dirksen Bussiere, Molly Min He, Johanna M Jansen, Gena Lapointe, Sylvia Ma, Jayesh Vora, Marion Wiesmann

Affiliation

¹ Small Molecule Drug Discovery, Biopharma Division, Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA.

PMID: 16446087
DOI: 10.1016/j.bmcl.2006.01.020

Abstract

Herein are described a series of novel heterocyclic analogs of the 4-amino-3-benzimidazol-2-ylhydroquinolin-2-one scaffold. These compounds are potent inhibitors of receptor tyrosine kinases and exhibit favorable pharmacokinetic profiles. The synthesis and SAR of these compounds are described.

MeSH terms

Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology
Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Heterocyclic Compounds / chemical synthesis*
Heterocyclic Compounds / pharmacology
Hydroquinones / chemical synthesis*
Hydroquinones / pharmacology
Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzimidazoles
Enzyme Inhibitors
Heterocyclic Compounds
Hydroquinones
Receptor Protein-Tyrosine Kinases