当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.

Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.

Abstract：

:Continuous efforts in microwave-assisted synthesis and the structure-activity relationships' (SARs) studies of novel modified 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitriles, allowed identification of new amidine and imidate derivatives as potent and dual CDK1/GSK-3 inhibitors. Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Logé C,Testard A,Thiéry V,Lozach O,Blairvacq M,Robert JM,Meijer L,Besson T

doi

10.1016/j.ejmech.2007.09.020

subject

Has Abstract

pub_date

2008-07-01 00:00:00

pages

1469-77

issue

7

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00355-8

journal_volume

43

pub_type

杂志文章

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