Synthesis and evaluation of the antiproliferative activity of novel thiazoloquinazolinone kinases inhibitors.
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.
Testard
Alexandra
A
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
Picot
Laurent
L
Lozach
Olivier
O
Blairvacq
Melina
M
Meijer
Laurent
L
Murillo
Laurence
L
Piot
Jean-Marie
JM
Thiéry
Valérie
V
Besson
Thierry
T
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
D004791:Enzyme Inhibitors; D011799:Quinazolines; D018844:Cyclin-Dependent Kinases; D038362:Glycogen Synthase Kinase 3