Discovery of C‑5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1

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成果类型：

期刊论文

作者：

Lang, Jia-Jia;Lv, You;Kobe, Bostjan;Chen, Hongfei;Tan, Yan;...

通讯作者：

Mi, Pengbing;Zheng, Xing;Lin, YW

作者机构：

[Lang, Jia-Jia; Mi, Pengbing; Lin, Ying-Wu; Zheng, Xing; Zheng, X] Univ South China, Hengyang Med Coll, Sch Chem & Chem Engn, Hengyang 421001, Peoples R China.

[Tan, Yan; Mi, Pengbing; Lin, Ying-Wu; Chen, Limei; Zheng, Xing; Chen, Hongfei; Zheng, X] Univ South China, Hengyang Med Sch, Dept Pharm, Hengyang 421001, Hunan, Peoples R China.

[Lang, Jia-Jia; Mi, Pengbing; Lin, Ying-Wu] Univ South China, Key Lab Prot Struct & Funct Univ Hunan Prov, Hengyang 421001, Peoples R China.

[Wang, Xuechuan; Lv, You] Univ Sci & Technol, Coll Bioresources Chem & Mat Engn, Xian 710021, Shaanxi, Peoples R China.

[Lv, You] Xian Amazinggene Co Ltd, Xian 710026, Shaanxi, Peoples R China.

通讯机构：

[Mi, PB; Lin, YW ; Zheng, X] U

Univ South China, Hengyang Med Sch, Dept Pharm, Hengyang 421001, Hunan, Peoples R China.

Univ South China, Hengyang Med Coll, Sch Chem & Chem Engn, Hengyang 421001, Peoples R China.

Univ South China, Key Lab Prot Struct & Funct Univ Hunan Prov, Hengyang 421001, Peoples R China.

语种：

英文

期刊：

JOURNAL OF MEDICINAL CHEMISTRY

ISSN：

0022-2623

年：

2023

卷：

期：

页码：

6725-6742

DOI：

10.1021/acs.jmedchem.3c00050

基金类别：

Natural Science Foundation of Hunan Province [2021JJ40451]; Research Foundation of Education Department of Hunan Province [21C0283, 21C0290]; Research Foundation of Health Commission of Hunan Province [202113050308]; University of South China [190XQD142]

机构署名：

本校为第一且通讯机构

院系归属：

化学化工学院

药学与生物科学学院

摘要：

Developing selective inhibitors for Janus kinase 1 (JAK1) is a significant focus for improving the efficacy and alleviating the adverse effects in treating immune-inflammatory diseases. Herein, we report the discovery of a series of C-5 pyrazole-modified pyrrolopyrimidine derivatives as JAK1-selective inhibitors. The potential hydrogen bond between the pyrazole group and E966 in JAK1 is the key point that enhances JAK1 selectivity. These compounds exhibit 10- to 20-fold JAK1 selectivity over JAK2 in enzyme assays. Compound 12b also exhibits excellent JAK1 selectivity in Ba/F3-TEL-JAK cellular ...

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Discovery of C‑5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1

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