Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue ARKIVOC - Online Journal of Organic Chemistry Année : 2020

Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position

Résumé

As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.

Domaines

Chimie

Dates et versions

hal-02926291 , version 1 (31-08-2020)

Identifiants

Citer

Yannick Esvan, Béatrice Josselin, Blandine Baratte, Stéphane Bach, Sandrine Ruchaud, et al.. Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position. ARKIVOC - Online Journal of Organic Chemistry, 2020, 2020 (7), pp.105-116. ⟨10.24820/ark.5550190.p011.268⟩. ⟨hal-02926291⟩
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