Design, synthesis, and testing of an isoquinoline-3-carboxylic-based novel anti-tumor lead

被引：14

作者：

Gao, Fei ^{[1
]}

Liu, Haiqing ^{[1
]}

Li, Li ^{[1
]}

Guo, Jianpeng ^{[1
]}

Wang, Yuji ^{[1
]}

Zhao, Ming ^{[1
,2
]}

Peng, Shiqi ^{[1
]}

机构：

[1] Capital Med Univ, Beijing Lab Biomed Mat, Beijing Area Major Lab Peptide & Small Mol Drugs, Engn Res Ctr,Minist Educ China,Coll Pharmaceut Sc, Beijing 100069, Peoples R China

[2] Kaohsiung Med Univ, Fac Biomed Sci & Environm Biol, Kaohsiung, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 20期

基金：

北京市自然科学基金; 中国国家自然科学基金;

关键词：

Isoquinoline-3-carboxylic acid; Anti-tumor; Benzoic acid; Multiple pharmacophores; Tris(2-aminoethyl)amine; POTENT; ANTAGONISTS; INHIBITORS;

D O I：

10.1016/j.bmcl.2015.09.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Compound 6, a novel isoquinoline comprising two isoquinoline-3-carboxylic acids and a benzoic acid conjugated together using tris(2-aminoethyl) amine, was synthesized and tested for anti-tumor activity. In vivo evaluations found 6 to be well tolerated, of high therapeutic efficacy and of low systemic toxicity, at effective doses. The results suggest 6 to be a promising lead for future study, and the use of multiple isoquinoline-3-carboxylic acid moieties as pharmacophores in the same molecule to be a useful strategy for the design of anti-tumor drugs. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4434 / 4436

页数：3

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