title: Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.
abstract: New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523.
authors.affiliation: Bristol-Myers Squibb Company, Experimental Station, PO Box 80500, Wilmington, DE 19880-0500, USA. eddyyue@incyte.com
authors.forename: Eddy W
authors.initials: EW
authors.lastname: Yue
authors.forename: Susan V
authors.initials: SV
authors.lastname: DiMeo
authors.forename: C Anne
authors.initials: CA
authors.lastname: Higley
authors.forename: Jay A
authors.initials: JA
authors.lastname: Markwalder
authors.forename: Catherine R
authors.initials: CR
authors.lastname: Burton
authors.forename: Pamela A
authors.initials: PA
authors.lastname: Benfield
authors.forename: Robert H
authors.initials: RH
authors.lastname: Grafstrom
authors.forename: Sarah
authors.initials: S
authors.lastname: Cox
authors.forename: Jodi K
authors.initials: JK
authors.lastname: Muckelbauer
authors.forename: Angela M
authors.initials: AM
authors.lastname: Smallwood
authors.forename: Haiying
authors.initials: H
authors.lastname: Chen
authors.forename: Chong Hwan
authors.initials: CH
authors.lastname: Chang
authors.forename: George L
authors.initials: GL
authors.lastname: Trainor
authors.forename: Steven P
authors.initials: SP
authors.lastname: Seitz
mesh_terms: D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005347:Fibroblasts / Q000187:drug effects / Q000201:enzymology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D011720:Pyrazoles; D018844:Cyclin-Dependent Kinases