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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

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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.
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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