Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors

J Enzyme Inhib Med Chem. 2005 Dec;20(6):557-68. doi: 10.1080/14756360500212399.

Abstract

The microwave-assisted synthesis of a family of 2,8-substituted thiazoloquinazolinones is described. The preliminary evaluation of the antiproliferative activity and the capacity of these molecules to inhibit CDKs and GSK-3 are reported. A lead compound was identified, constituting a scaffold from which more potent inhibitors could be designed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / radiation effects
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Humans
  • Microwaves
  • Molecular Structure
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology*
  • Quinazolines / radiation effects
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Quinazolines
  • Cyclin-Dependent Kinases
  • Glycogen Synthase Kinase 3