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

Marine Drugs

Anna Carbone²  Barbara Parrino²  Paola Barraja²  Virginia Spanò²  Girolamo Cirrincione²  Patrizia Diana²  Armin Maier¹  Gerhard Kelter¹ 

[1] Oncotest GmbH, Institute for Experimental Oncology, Am Flughafen 12-14, 79108 Freiburg, Germany; E-Mails:;Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, STEBICEF, via Archirafi 32, 90123-Palermo, Italy; E-Mails:

关键词: bis-indolyl-pyrroles;    nortopsentin analogues;    marine alkaloids;    antitumor;    ex-vivo xenografts;   

DOI  :  10.3390/md11030643

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.