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N-（芳基）-4-（唑基乙基）噻唑-5-甲酰胺：新型强效血管内皮生长因子受体I和II抑制剂

N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.

作者信息

Kiselyov Alexander S, Piatnitski Evgueni, Semenova Marina, Semenov Victor V

机构信息

Small Molecule Drug Discovery, Chemical Diversity, Inc., 11558 Sorrento Valley Road, San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2006 Feb;16(3):602-6. doi: 10.1016/j.bmcl.2005.10.058. Epub 2005 Nov 3.

DOI:10.1016/j.bmcl.2005.10.058
PMID:16275072
Abstract

Novel potent derivatives of N-(aryl)-4-(azolylethyl)thiazole-5-carboxamides are described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC(50)<100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido pharmacophore, both dual and specific VEGFR-2 thiazoles were identified.

摘要

N-（芳基）-4-（唑基乙基）噻唑-5-甲酰胺的新型强效衍生物被描述为血管内皮生长因子受体II（VEGFR-2）的抑制剂。在酶促和细胞试验中，几种化合物显示出VEGFR-2抑制活性，IC（50）<100 nM。这些化合物还抑制相关的酪氨酸激酶VEGFR-1。通过控制5-甲酰胺基药效团上的取代模式，鉴定出了双重和特异性VEGFR-2噻唑。

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