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

✍ Scribed by Jin-Jun Liu; Irena Daniewski; Qingjie Ding; Brian Higgins; Grace Ju; Kenneth Kolinsky; Fred Konzelmann; Christine Lukacs; Giacomo Pizzolato; Pamela Rossman; Amy Swain; Kshitij Thakkar; Chung-Chen Wei; Dorota Miklowski; Hong Yang; Xuefeng Yin; Peter M. Wovkulich

Book ID: 104004802
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 472 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.079

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✦ Synopsis

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.

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