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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Synthesis and Cytotoxic Activity of New β-Carboline Derivatives

Author(s): A. Peduto, V. More, P. de Caprariis, M. Festa, A. Capasso, S. Piacente, L. De Martino, V. De Feo and R. Filosa

Volume 11, Issue 6, 2011

Page: [486 - 491] Pages: 6

DOI: 10.2174/138955711795843383

Price: $65


On the basis of harmine and 1-methoxy-canthin-6-one chemical structures, a series of novel 1,4-disubstituted and 1,4,9-trisubstituted β-carbolines and tetracyclic derivatives were designed and synthesized. Cytotoxic activities of these compounds in vitro were investigated in a human tumor cell line panel. Almost all compounds demonstrated interesting cytotoxic activities in particular against prostate cancer cells PC-3 with IC50 in the low micromolar range. Compound X was found to be the most potent one with IC50 value of 8.0 μM; this suggests further studies with models of prostate cancer.

Keywords: β-carbolines, 1-methoxycanthin-6-one, prostate cancer, harmine, Cytotoxic, 1,4,9-trisubstituted, 1,4-disubstituted, alkaloids, herbal drug, antitumor

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