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

Alexandra Testard, Laurent Picot, Olivier Lozach, Mélina Blairvacq, Laurent Meijer, Laurence Murillo, Jean‐Marie Piot, Valérie Thiéry, Thierry Besson

Journal of Enzyme Inhibition and Medicinal Chemistry · 2005 · 38 citations · 10 references

Concepts

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.

References

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