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Bioorg Med Chem Lett ; 17(13): 3618-23, 2007 Jul 01.
Article in English | MEDLINE | ID: mdl-17490879

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.


Subject(s)
Antineoplastic Agents/pharmacokinetics , Chemistry, Pharmaceutical/methods , Drug Screening Assays, Antitumor , Protein Kinase Inhibitors/pharmacokinetics , Protein Kinases/chemistry , Animals , Antineoplastic Agents/chemistry , Caco-2 Cells , Checkpoint Kinase 1 , DNA Damage , Drug Design , Flow Cytometry , Humans , Inhibitory Concentration 50 , Mice , Microsomes, Liver/metabolism , Protein Kinase Inhibitors/chemistry , Protein Kinases/metabolism , Rats
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