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Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.

Abstract：

:We disclose a novel series of indenopyrazole-based cyclin-dependent kinase (CDK) inhibitors. Kinetic experiments confirmed our initial molecular modeling studies that the compounds are competitive with respect to adenosine 5'-triphosphate (ATP) and bind in the kinase ATP pocket. A unique combination of active pharmacophores led us to a series of semicarbazide-based inhibitors that are highly potent against CDK2 and CDK4 while maintaining selectivity against other relevant serine/threonine kinases. These compounds were active against a transformed human colon cancer cell line (HCT116) while maintaining an acceptable margin of activity against a normal fibroblast cell line. The compounds were found to be highly protein bound in our cell-based assay with the exception of 11k, which maintained a reasonable level of activity in the presence of human plasma proteins.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Nugiel DA,Vidwans A,Etzkorn AM,Rossi KA,Benfield PA,Burton CR,Cox S,Doleniak D,Seitz SP

doi

10.1021/jm020171+

keywords:

subject

Has Abstract

pub_date

2002-11-21 00:00:00

pages

5224-32

issue

24

eissn

0022-2623

issn

1520-4804

pii

jm020171+

journal_volume

45

pub_type

杂志文章

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