3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors

Christopher M McBride; Paul A Renhowe; Thomas G Gesner; Johanna M Jansen; Julie Lin; Sylvia Ma; Yasheen Zhou; Cynthia M Shafer

doi:10.1016/j.bmcl.2006.04.043

3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3789-92. doi: 10.1016/j.bmcl.2006.04.043. Epub 2006 May 5.

Authors

Christopher M McBride¹, Paul A Renhowe, Thomas G Gesner, Johanna M Jansen, Julie Lin, Sylvia Ma, Yasheen Zhou, Cynthia M Shafer

Affiliation

¹ Small Molecule Drug Discovery, Medicinal Chemistry Department, Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA.

PMID: 16678414
DOI: 10.1016/j.bmcl.2006.04.043

Abstract

The 3-benzimidazol-2-yl-1H-indazole scaffold was developed as an alternate scaffold for our receptor tyrosine kinase (RTK) inhibitor program. In exploring the SAR of this series, it was discovered that a subset of these compounds potently inhibit the enzyme c-ABL. The SAR of these compounds is described.

MeSH terms

Benzimidazoles / chemical synthesis
Benzimidazoles / pharmacology
Cell Proliferation / drug effects*
Cells, Cultured
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Humans
Indazoles / chemical synthesis*
Indazoles / pharmacology*
Proto-Oncogene Proteins c-abl / antagonists & inhibitors*
Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzimidazoles
Enzyme Inhibitors
Indazoles
Receptor Protein-Tyrosine Kinases
Proto-Oncogene Proteins c-abl