Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy

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成果类型：

期刊论文

作者：

Zhuo, Linsheng*;Guo, Mengqin;Zhang, Siyi;Wu, Junbo;Wang, Mingshu;...

通讯作者：

Zhuo, LS;Huang, W;Zhuo, Linsheng;Jiang, WF

作者机构：

[Zhuo, Linsheng; Shen, Yang; Zhuo, LS] Univ South China, Hengyang Med Sch, Postdoctoral Stn Basic Med, Hengyang 421001, Hunan, Peoples R China.

[Wang, Mingshu; Huang, Wei] Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensor Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

[Peng, Xue; Wang, Zhen; Jiang, Weifan; Zhuo, Linsheng; Zhuo, LS; Zhang, Siyi] Univ South China, Sch Pharmaceut Sci, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.

[Wu, Junbo] Hengyang Cent Hosp, Dept Colorectal Surg, Hengyang 421001, Hunan, Peoples R China.

[Guo, Mengqin] Wuhan Univ, Sch Pharmaceut Sci, Wuhan 430071, Hubei, Peoples R China.

通讯机构：

[Huang, W ] C

[Zhuo, LS ; Jiang, WF ; Zhuo, LS] U

Univ South China, Hengyang Med Sch, Postdoctoral Stn Basic Med, Hengyang 421001, Hunan, Peoples R China.

Cent China Normal Univ, Coll Chem, Int Joint Res Ctr Intelligent Biosensor Technol &, Key Lab Pesticide & Chem Biol,Minist Educ, Wuhan 430079, Peoples R China.

Univ South China, Sch Pharmaceut Sci, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.

语种：

英文

关键词：

1,6-Naphthyridone;AXL kinase inhibitor;Kinase selectivity;Quinazoline

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2024

卷：

265

页码：

116090

DOI：

10.1016/j.ejmech.2023.116090

基金类别：

CRediT authorship contribution statement Linsheng Zhuo: Formal analysis, Investigation, Writing – original draft, Writing – review & editing. Mengqin Guo: Data curation, Formal analysis, Investigation, Software. Siyi Zhang: Conceptualization, Formal analysis, Resources. Junbo Wu: Resources. Mingshu Wang: Data curation, Investigation. Yang Shen: Resources. Xue Peng: Resources. Zhen Wang: Resources. Weifan Jiang: Conceptualization, acquisition, Resources, Software, Supervision. Wei Huang: Conceptualization, acquisition,

机构署名：

本校为通讯机构

院系归属：

化学学院

摘要：

The role of AXL in various oncogenic processes has made it an attractive target for cancer therapy. Currently, kinase selectivity profiles, especially circumventing MET inhibition, remain a scientific issue of great interest in the discovery of selective type II AXL inhibitors. Starting from a dual MET/AXL-targeted lead structure from our previous work, we optimized a 1,6-naphthyridinone series using molecular modeling-assisted compound design to improve AXL potency and selectivity over MET, resulting in the potent and selective type II AXL-targeted compound 25c. This showed excellent AXL inhi...

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Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy

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