Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. doi: 10.1016/j.bmcl.2006.03.069. Epub 2006 Apr 5.

Authors

Christopher M McBride¹, Paul A Renhowe, Carla Heise, Johanna M Jansen, Gena Lapointe, Sylvia Ma, Ramon Piñeda, Jayesh Vora, Marion Wiesmann, Cynthia M Shafer

Affiliation

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

PMID: 16603352
DOI: 10.1016/j.bmcl.2006.03.069

Abstract

3-Benzimidazol-2-yl-1H-indazole analogs were developed as inhibitors of receptor tyrosine kinases (RTK). The synthesis and SAR of this series is reported.

MeSH terms

Animals
Benzimidazoles / chemical synthesis*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug Design
Indazoles / chemical synthesis*
Indazoles / chemistry
Indazoles / pharmacology*
Mice
Mice, Nude
Models, Molecular
Molecular Structure
Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
Stereoisomerism
Structure-Activity Relationship

Substances

Benzimidazoles
Indazoles
Receptor Protein-Tyrosine Kinases