Synthesis and Cytotoxic Activity of New β-Carboline Derivatives

Title: Synthesis and Cytotoxic Activity of New β-Carboline Derivatives

Volume: 11 Issue: 6

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Peduto A., More V., de Caprariis P., Festa M., Capasso A., Piacente S., De Martino L., De Feo V. and Filosa R., Synthesis and Cytotoxic Activity of New β-Carboline Derivatives, Mini-Reviews in Medicinal Chemistry 2011; 11 (6) . https://dx.doi.org/10.2174/138955711795843383