Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3

Bioorganic & Medicinal Chemistry Letters
Alexandra TestardThierry Besson

Abstract

In an effort to identify new protein kinase inhibitors with increased potency and selectivity, we have developed the microwave-assisted synthesis of thiazolo[5,4-f]quinazolin-9-ones. The effects of eighteen derivatives on CDK1/cyclin B, CDK5/p25, and GSK-3 were investigated. Several turned out to inhibit GSK-3 in the micromolar range. Molecular modeling studies suggest that the most selective GSK-3 inhibitors 7a-d bind into the ATP-binding site through a key hydrogen bond interaction with Val135 and target the specific hydrophobic backpocket of the enzyme.

References

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Citations

Mar 3, 2012·Organic and Medicinal Chemistry Letters·Mahendra KumarDinesh Kumar Sharma
Oct 1, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alicia FoucourtThierry Besson
Sep 30, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alicia FoucourtThierry Besson
Apr 16, 2009·British Journal of Pharmacology·Geetha Vani RayasamAbhijit Ray
Mar 26, 2014·Nucleosides, Nucleotides & Nucleic Acids·Dhaval D HaveliwalaSaurabh K Patel
May 6, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Damien HédouThierry Besson
Jun 21, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Damien HédouThierry Besson
Aug 31, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Florence CoulyThierry Besson
Nov 27, 2007·Journal of Enzyme Inhibition and Medicinal Chemistry·Maria De Fatima PereiraThierry Besson
Jan 16, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ebraheem Abdu Musad SalehK M Lokanatha Rai
Feb 14, 2013·ACS Medicinal Chemistry Letters·Rémi GuillonPatrice Le Pape

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