Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity

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成果类型：

期刊论文

作者：

Chen, Limei*;Tang, Yahua;Lang, Jia-Jia;Lin, Yuqing;Yu, Zhixin;...

通讯作者：

Chen, Limei;Mi, PB;Lin, YW;Lv, Y

作者机构：

[Chen, Limei; Zheng, Xing; Chen, LM; Li, Xinhao; Mi, Pengbing; Yu, Zhixin; Lin, Yuqing] Univ South China, Dept Pharm, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.

[Tang, Yahua] Univ South China, Affiliated Nanhua Hosp, Inst Clin Pharm, Hengyang Med Sch,Dept Pharm, Hengyang 421001, Hunan, Peoples R China.

[Lang, Jia-Jia; Lin, Ying-Wu] Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.

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

[Zheng, Xing] Hunan Vocat Coll Sci & Technol, Dept Pharm, Changsha 410004, Hunan, Peoples R China.

通讯机构：

[Chen, LM; Lin, YW ; Mi, PB ] U

[Lv, Y ] S

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

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

Shaanxi Univ Sci & Technol, Coll Bioresources Chem & Mat Engn, Xian 710021, Shaanxi, Peoples R China.

语种：

英文

关键词：

Autoimmune diseases;JAK-STAT pathway;JAK1-Selective inhibitor;Orthogonal strategy;Pyrrolopyridine skeleton

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2024

卷：

267

页码：

116210

DOI：

10.1016/j.ejmech.2024.116210

基金类别：

CRediT authorship contribution statement Limei Chen: Data curation. Yahua Tang: Formal analysis. Jia-Jia Lang: acquisition, Formal analysis. Yuqing Lin: Data curation. Zhixin Yu: Methodology, Formal analysis, Data curation. Xinhao Li: Methodology. Xing Zheng: Writing – review & editing, acquisition. Pengbing Mi: Writing – review & editing, Writing – original draft, Conceptualization. You Lv: Writing – review & editing, Writing – original draft. Ying-Wu Lin: Writing – review & editing. Acknowledgments The authors thank The Health Research Project of Hunan Provincial Health Commission (202113050308, 20231438), The initial funding of University of South China (190XQD142), Hunan Province Training Program of Innovation and Entrepreneurship for Undergraduates (S202210555283) and University of South China Training Program of Innovation and Entrepreneurship for Undergraduates (D202305111158095145) for financial support.

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：

The development of highly selective Janus Kinase 1 (JAK1) inhibitors is crucial for improving efficacy and minimizing adverse effects in the clinical treatment of autoimmune diseases. In a prior study, we designed a series of C-5 4-pyrazol substituted pyrrolopyridine derivatives that demonstrated significant potency against JAK1, with a 10∼20-fold selectivity over Janus Kinase 2 (JAK2). Building on this foundation, we adopted orthogonal strategy by modifying the C-5 position with 3-pyrazol/4-pyrazol/3-pyrrol groups and tail with substituted be...

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Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity

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