Design, synthesis, and evaluation of 2-methyl-and 2-amino-N-aryl-4, 5-dihydrothiazolo [4, 5-h] quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl) …

…, G Griffiths, AL Barnett, G Kontopidis…

Index: McIntyre, Neil A.; McInnes, Campbell; Griffiths, Gary; Barnett, Anna L.; Kontopidis, George; Slawin, Alexandra M. Z.; Jackson, Wayne; Thomas, Mark; Zheleva, Daniella I.; Wang, Shudong; Blake, David G.; Westwood, Nicholas J.; Fischer, Peter M. Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2136 - 2145

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Citation Number: 21

Abstract

Following the recent discovery and development of 2-anilino-4-(thiazol-5-yl) pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring- constrained analogues, specifically, 2-methyl-and 2-amino-N-aryl-4, 5-dihydrothiazolo [4, 5- h] quinazolin-8-amines for inhibition of CDKs. Here we report the rational design, synthesis, structure− activity relationships (SARs), and cellular mode-of-action profile of these ...