title: Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors.
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.
authors.affiliation: Laboratoire de Biotechnologies et Chimie Bio-organique, FRE CNRS 2766, UFR Sciences Fondamentales et Sciences pour l'Ingenieur, Bâtiment Marie Curie, Université de la Rochelle, F-l 7042 La Rochelle cedex 1, France
authors.forename: Alexandra
authors.initials: A
authors.lastname: Testard
authors.forename: Laurent
authors.initials: L
authors.lastname: Picot
authors.forename: Olivier
authors.initials: O
authors.lastname: Lozach
authors.forename: Melina
authors.initials: M
authors.lastname: Blairvacq
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Laurence
authors.initials: L
authors.lastname: Murillo
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Piot
authors.forename: Valérie
authors.initials: V
authors.lastname: Thiéry
authors.forename: Thierry
authors.initials: T
authors.lastname: Besson
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000528:radiation effects; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D006801:Humans; D008872:Microwaves; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000528:radiation effects; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011799:Quinazolines; D018844:Cyclin-Dependent Kinases; D038362:Glycogen Synthase Kinase 3