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氨基吡啶甲酰胺作为c-Jun氨基末端激酶抑制剂：靶向守门残基及其他。

Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.

作者信息

Liu Gang, Zhao Hongyu, Liu Bo, Xin Zhili, Liu Mei, Kosogof Christi, Szczepankiewicz Bruce G, Wang Sanyi, Clampit Jill E, Gum Rebecca J, Haasch Deanna L, Trevillyan James M, Sham Hing L

机构信息

Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6101, USA.

出版信息

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5723-30. doi: 10.1016/j.bmcl.2006.08.097. Epub 2006 Sep 12.

DOI:10.1016/j.bmcl.2006.08.097
PMID:16971120
Abstract

The structure-activity relationships of 5,6-positions of aminopyridine carboxamide-based c-Jun N-terminal Kinase (JNK) inhibitors were explored to expand interaction with the kinase specificity and ribose-binding pockets. The syntheses of analogues and the impact of structural modification on in vitro potency and cellular activity are described.

摘要

为了扩大与激酶特异性口袋和核糖结合口袋的相互作用，对基于氨基吡啶甲酰胺的c-Jun氨基末端激酶（JNK）抑制剂5,6位的构效关系进行了研究。本文描述了类似物的合成以及结构修饰对体外效力和细胞活性的影响。

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