2. Academic Validation
  3. Synthesis and biological evaluation of 1,9-disubstituted β-carbolines as potent DNA intercalating and cytotoxic agents

Synthesis and biological evaluation of 1,9-disubstituted β-carbolines as potent DNA intercalating and cytotoxic agents

  • Eur J Med Chem. 2011 Oct;46(10):5127-37. doi: 10.1016/j.ejmech.2011.08.027.
Zhiyong Chen 1,  Rihui Cao,  Buxi Shi,  Liang Guo,  Jie Sun,  Qin Ma,  Wenxi Fan,  Huacan Song
Affiliations

Affiliation

  • 1 Guangdong Provincial Public Laboratory of Analysis and Testing Technology, China National Analytical Center, Building 34, 100 Xianlie Middle Road, Guangzhou, 510070, PR China.
PMID: 21875764 DOI: 10.1016/j.ejmech.2011.08.027
Abstract

A series of novel 1,9-disubstituted β-carbolines was designed, synthesized and evaluated as cytotoxic and DNA intercalating agents. Compounds 7b, 7c, 8b and 8c exhibited the most potent cytotoxic activities with IC(50) values of lower than 20 μM against ten human tumor cell lines. The results indicated that (1) the 3-chlorobenzyl and 3-phenylpropyl substituents in position-9 of β-carboline nucleus were the suitable pharmacophoric group giving rise to significant antitumor agents; (2) the length of the alkylamino side chain moiety affected their cytotoxic potencies, and three CH(2) units were more favorable. In addition, these compounds were found to exhibit remarkable DNA intercalating effects.

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