| Literature DB >> 17490879 |
Yunsong Tong1, Akiyo Claiborne, Magdalena Pyzytulinska, Zhi-Fu Tao, Kent D Stewart, Peter Kovar, Zehan Chen, Robert B Credo, Ran Guan, Philip J Merta, Haiying Zhang, Jennifer Bouska, Elizabeth A Everitt, Bernard P Murry, Dean Hickman, Tim J Stratton, Jian Wu, Saul H Rosenberg, Hing L Sham, Thomas J Sowin, Nan-horng Lin.
Abstract
A study on substitutions at the four open positions on the phenyl ring of the 1,4-dihydroindeno[1,2-c]pyrazoles as potent CHK-1 inhibitors is described. Bis-substitution at both the 6- and 7-positions led to inhibitors with IC(50) values below 0.3nM. The compound with the best overall activities (36) was able to potentiate the anti-proliferative effect of doxorubicin in HeLa cells by at least 47-fold. Physicochemical, metabolic, and pharmacokinetic properties of selected inhibitors are also disclosed.Entities:
Mesh：
Substances：
Year: 2007 PMID： 17490879 DOI： 10.1016/j.bmcl.2007.04.055
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823