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7188547 
Journal Article 
Design, synthesis, and testing of an isoquinoline-3-carboxylic-based novel anti-tumor lead 
Gao, F; Liu, H; Li, L; Guo, J; Wang, Y; Zhao, M; Peng, S; , 
2015 
Yes 
Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405 
PERGAMON-ELSEVIER SCIENCE LTD 
OXFORD 
25 
20 
4434-4436 
English 
26386603 
WOS:000362102200011 
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. 
Antineoplastic Agents; Benzoates; Isoquinolines; isoquinoline-3-carboxylic acid; Index Medicus; Benzoic acid; Multiple pharmacophores; Anti-tumor; Tris(2-aminoethyl)amine; Structure-Activity Relationship; Benzoates -- chemical synthesis; Dose-Response Relationship, Drug; Cell Proliferation -- drug effects; Animals; Neoplasms, Experimental -- pathology; Cell Line, Tumor; Benzoates -- pharmacology; Benzoates -- chemistry; Molecular Structure; Neoplasms, Experimental -- drug therapy; Drug Screening Assays, Antitumor; Antineoplastic Agents -- pharmacology; Antineoplastic Agents -- chemical synthesis; Antineoplastic Agents -- chemistry; Drug Design; Isoquinolines -- chemical synthesis; Isoquinolines -- pharmacology; Isoquinolines -- chemistry