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

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.

• Authors: Fei Gao, Haiqing Liu, Li Li, Jianpeng Guo, Yuji Wang, Ming Zhao, Shiqi Peng
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 25 Issue 20 Pg. 4434-6 (Oct 15 2015) ISSN: 1464-3405 [Electronic] England
• PMID: 26386603 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Benzoates
• Isoquinolines
• isoquinoline-3-carboxylic acid

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Benzoates (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Design
• Drug Screening Assays, Antitumor
• Humans
• Isoquinolines (chemical synthesis, chemistry, pharmacology)
• Mice
• Molecular Structure
• Neoplasms, Experimental (drug therapy, pathology)
• Structure-Activity Relationship