Mar. Drugs 2013, 11(3), 643-654; doi:10.3390/md11030643
Article

Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

1 Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, STEBICEF, via Archirafi 32, 90123-Palermo, Italy 2 Oncotest GmbH, Institute for Experimental Oncology, Am Flughafen 12-14, 79108 Freiburg, Germany
* Author to whom correspondence should be addressed.
Received: 21 December 2012; in revised form: 22 January 2013 / Accepted: 6 February 2013 / Published: 1 March 2013
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Abstract: 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.
Keywords: bis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenografts

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MDPI and ACS Style

Carbone, A.; Parrino, B.; Barraja, P.; Spanò, V.; Cirrincione, G.; Diana, P.; Maier, A.; Kelter, G.; Fiebig, H.-H. Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin. Mar. Drugs 2013, 11, 643-654.

AMA Style

Carbone A, Parrino B, Barraja P, Spanò V, Cirrincione G, Diana P, Maier A, Kelter G, Fiebig H-H. Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin. Marine Drugs. 2013; 11(3):643-654.

Chicago/Turabian Style

Carbone, Anna; Parrino, Barbara; Barraja, Paola; Spanò, Virginia; Cirrincione, Girolamo; Diana, Patrizia; Maier, Armin; Kelter, Gerhard; Fiebig, Heinz-Herbert. 2013. "Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin." Mar. Drugs 11, no. 3: 643-654.

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