Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability

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期刊论文

作者：

Xu, Juan;Zhao, Anmin;Chen, Danni;Wang, Jiao;Ma, Jirui;...

通讯作者：

He, Huan;Pan, Weidong;Zhang, SL

作者机构：

[Chen, Danni; Wang, Jiao; Ma, Jirui; Xu, Juan; Zhao, Anmin] Hubei Polytech Univ, Coll Chem & Chem Engn, Hubei Key Lab Mine Environm Pollut Control & Remed, Huangshi 435003, Peoples R China.

[Zhang, Silong; Pan, Weidong; Qing, Luolong; He, Huan; He, H; Zhang, SL] Guizhou Univ, Sch Pharmaceut Sci, Key Lab Plant Resource Conservat & Germplasm Innov, Minist Educ, Guiyang 550025, Peoples R China.

[Li, Yuanyuan] Wuhan Polytech Univ, Sch Life Sci & Technol, Wuhan 430023, Peoples R China.

[Zhang, Silong; Li, Yuanyuan; Fang, Huaxiang; He, Huan; Xu, Juan] Wuhan Yuxiang Pharmaceut Technol Co Ltd, Wuhan 430200, Peoples R China.

通讯机构：

[He, H; Pan, WD; Zhang, SL ] G

Guizhou Univ, Sch Pharmaceut Sci, Key Lab Plant Resource Conservat & Germplasm Innov, Minist Educ, Guiyang 550025, Peoples R China.

语种：

英文

关键词：

ADME-T;Cyclization;PARP7;Pharmacokinetic;Selectivity

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2024

卷：

266

页码：

116160

DOI：

10.1016/j.ejmech.2024.116160

基金类别：

National Natural Science Foundation of China [82304310, 82204214, 22363002]; Natural Science Foundation of Hubei Province of China [2023AFB457]; Hubei Polytechnic University Startup Foundation for Advanced Talent [21XJZ03R]; College Student Innovation and Entrepreneurship Project of Hubei Polytechnic University [20221092003]; Wuhan Yuxiang Pharmaceutical Technology Co., Ltd.

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摘要：

PARP7 has been recently identified as an effective drug target due to its specific role in tumor generation and immune function recovery. Herin, we report the discovery of compound 8, which contained a tricyclic fused ring, as a highly selective PARP7 inhibitor against other PARPs. In particular, compound 8 strongly inhibits PARP7 with an IC(50) of 0.11nM, and suppresses the proliferation of NCI-H1373 lung cancer cells with an IC(50) of 2.5nM. Compound 8 exhibits a favorable pharmacokinetic profile with a bioavailability of 104% in mice, and 78% in dogs. Importantly, daily treatment of 30mg/kg...

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Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability

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