期刊
ARKIVOC
卷 -, 期 -, 页码 105-116出版社
ARKAT USA INC
DOI: 10.24820/ark.5550190.p011.268
关键词
Fused azines; isoquinolines; pyrimidines; pyridoquinazolines
资金
- Auvergne Region (Jeune Chercheur Program)
- French Ministry of Higher Education and Research
- Canceropole Grand Ouest (axis: natural sea products in cancer treatment)
- IBiSA (French Infrastructures in Life Science)
- Biogenouest (Western France Life Science and Environment Core Facility Network)
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. [GRAPHICS]
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