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Synthesis and Cytotoxic Activity of New β-Carboline Derivatives

[ Vol. 11 , Issue. 6 ]


A. Peduto, V. More, P. de Caprariis, M. Festa, A. Capasso, S. Piacente, L. De Martino, V. De Feo and R. Filosa   Pages 486 - 491 ( 6 )


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.


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


Dipartimento di Scienze Farmaceutiche, Universita di Salerno, Via Ponte don Melillo, 84084 Fisciano (SA), Italy.

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