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 IC 50 in the low micromolar range. Compound X was found to be the most potent one with IC 50 value of 8.0 βM; this suggests further studies with models of prostate cancer.
Synthesis and Cytotoxic Activity of New beta-carboline Derivatives
PEDUTO, ANTONELLA;MORE, VIJAYKUMAR SHIUDAS;DE CAPRARIIS, Paolo;FESTA, MICHELA;CAPASSO, Anna;PIACENTE, Sonia;DE MARTINO, LAURA;DE FEO, Vincenzo;
2011-01-01
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 IC 50 in the low micromolar range. Compound X was found to be the most potent one with IC 50 value of 8.0 βM; this suggests further studies with models of prostate cancer.File in questo prodotto:
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