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合成并优化噻二唑衍生物作为新型的 c-Jun N-端激酶底物竞争抑制剂。

Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.

机构信息

Burnham Institute for Medical Research, La Jolla, CA 92037, USA.

出版信息

Bioorg Med Chem. 2010 Jan 15;18(2):590-6. doi: 10.1016/j.bmc.2009.12.013. Epub 2009 Dec 11.

DOI:10.1016/j.bmc.2009.12.013
PMID:20045647
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2818674/
Abstract

A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein kinase JNK. We report on the synthesis, characterization and evaluation of a series of compounds that resulted in the identification of potent and selective JNK inhibitors targeting its JIP-1 docking site.

摘要

我们设计了一系列噻二唑衍生物作为蛋白激酶 JNK 的潜在别构、底物竞争性抑制剂。我们报告了一系列化合物的合成、表征和评估，这些化合物的鉴定结果为 JNK 的 JIP-1 对接位点提供了有效的选择性 JNK 抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/3e492b3a0b36/nihms-164195-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/2c3982c7050f/nihms-164195-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/2133b74c914c/nihms-164195-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/0b800445fdce/nihms-164195-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/3e492b3a0b36/nihms-164195-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/2c3982c7050f/nihms-164195-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/2133b74c914c/nihms-164195-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/0b800445fdce/nihms-164195-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbce/2818674/3e492b3a0b36/nihms-164195-f0004.jpg

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