Structural highlights
Publication Abstract from PubMed
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.
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.,Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. Epub 2010 Aug 21. PMID:20832307[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM. Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors. Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. Epub 2010 Aug 21. PMID:20832307 doi:10.1016/j.bmcl.2010.08.079
