Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors |
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Authors: | Testard Alexandra Picot Laurent Lozach Olivier Blairvacq Melina Meijer Laurent Murillo Laurence Piot Jean-Marie Thiéry Valérie Besson Thierry |
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Affiliation: | Laboratoire de Biotechnologies et Chimie Bio-organique, FRE CNRS 2766, UFR Sciences Fondamentales et Sciences pour l'Ingenieur, Batiment Marie Curie, Université de la Rochelle, F-l 7042 La Rochelle cedex 1, France |
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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. |
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