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

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 / Revised: 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. View Full-Text
Keywords: bis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenografts bis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenografts
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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.

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