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

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

  • Bioorg Med Chem Lett. 2015 Oct 15;25(20):4434-6. doi: 10.1016/j.bmcl.2015.09.014.
Fei Gao 1,  Haiqing Liu 1,  Li Li 2,  Jianpeng Guo 1,  Yuji Wang 1,  Ming Zhao 3,  Shiqi Peng 1
Affiliations

Affiliations

  • 1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
  • 2 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China. Electronic address: renulee@ccmu.edu.cn.
  • 3 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China; Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan. Electronic address: mingzhao@bjmu.edu.cn.
PMID: 26386603 DOI: 10.1016/j.bmcl.2015.09.014
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.

Keywords

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

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