Literature DB >> 27469128

Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives.

Wael Zeinyeh1, Yannick J Esvan1, Lionel Nauton1, Nadège Loaëc2, Laurent Meijer2, Vincent Théry1, Fabrice Anizon1, Francis Giraud3, Pascale Moreau4.   

Abstract

The synthesis of new diversely substituted pyrido[3,4-g]quinazolines is described. The inhibitory potencies of prepared compounds toward a panel of five CMGC protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3), that are known to play a potential role in Alzheimer's disease, were evaluated. The best overall kinase inhibition profile was found for nitro compound 4 bearing an ethyl group at the 5-position.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  CDK5; CK1; CLK1; DYRK1A; GSK3; Protein kinase inhibition; Pyrido[3,4-g]quinazoline

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Year:  2016        PMID: 27469128     DOI: 10.1016/j.bmcl.2016.07.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  5-Methoxybenzothiophene-2-Carboxamides as Inhibitors of Clk1/4: Optimization of Selectivity and Cellular Potency.

Authors:  Ahmed K ElHady; Dalia S El-Gamil; Po-Jen Chen; Tsong-Long Hwang; Ashraf H Abadi; Mohammad Abdel-Halim; Matthias Engel
Journal:  Molecules       Date:  2021-02-13       Impact factor: 4.411

2.  Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines.

Authors:  Mathilde Defois; Chloé Rémondin; Béatrice Josselin; Lionel Nauton; Vincent Théry; Fabrice Anizon; Sandrine Ruchaud; Francis Giraud; Pascale Moreau
Journal:  Molecules       Date:  2022-08-30       Impact factor: 4.927

  2 in total

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