title: Synthesis and cytotoxic activity of new β-carboline derivatives.
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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte don Melillo, 84084 Fisciano (SA), Italy. apeduto@unisa.it
authors.forename: A
authors.initials: A
authors.lastname: Peduto
authors.forename: V
authors.initials: V
authors.lastname: More
authors.forename: P
authors.initials: P
authors.lastname: de Caprariis
authors.forename: M
authors.initials: M
authors.lastname: Festa
authors.forename: A
authors.initials: A
authors.lastname: Capasso
authors.forename: S
authors.initials: S
authors.lastname: Piacente
authors.forename: L
authors.initials: L
authors.lastname: De Martino
authors.forename: V
authors.initials: V
authors.lastname: De Feo
authors.forename: R
authors.initials: R
authors.lastname: Filosa
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000633:toxicity; D002243:Carbolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines