Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
- Autori: Carbone, A.; Parrino, B.; Barraja, P.; Spano', V.; Cirrincione, G.; Diana, P.; Maier, A.; Kelter, G.; Fiebig, H.
- Anno di pubblicazione: 2013
- Tipologia: Articolo in rivista (Articolo in rivista)
- Parole Chiave: bis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenografts
- OA Link: http://hdl.handle.net/10447/72063
2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.