Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. doi: 10.1016/j.bmcl.2010.08.079. Epub 2010 Aug 21.

Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

Author information

1
Discovery Chemistry, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. jin-jun.liu@roche.com

Abstract

A novel series of pyrazolobenzodiazepines 3 has been identified as potent inhibitors of cyclin-dependent kinase 2 (CDK2). Their synthesis and structure-activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK2 activity in vitro, and block cell cycle progression in human tumor cell lines. Further exploration has revealed that this class of compounds inhibits several kinases that play critical roles in cancer cell growth and division as well as tumor angiogenesis. Together, these properties suggest a compelling basis for their use as antitumor agents.

PMID:
20832307
DOI:
10.1016/j.bmcl.2010.08.079
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center