Design, synthesis, and testing of an isoquinoline-3-carboxylic-based novel anti-tumor lead. Issue 20 (15th October 2015)

• Record Type: Journal Article
• Authors: Gao, Fei; Liu, Haiqing; Li, Li; Guo, Jianpeng; Wang, Yuji; Zhao, Ming; Peng, Shiqi
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 20(2015)
• Page Start: 4434
• Page End: 4436
• Publication Date: 2015-10-15
• Subjects: Isoquinoline-3-carboxylic acid -- Anti-tumor -- Benzoic acid -- Multiple pharmacophores -- Tris(2-aminoethyl)amine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.09.014
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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. Abstract: 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.