Journal
MARINE DRUGS
Volume 11, Issue 3, Pages 643-654Publisher
MDPI AG
DOI: 10.3390/md11030643
Keywords
bis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenografts
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Funding
- Ministero dell'Istruzione dell'Universita e della Ricerca (MIUR)
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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 mu M and 0.67 mu M, 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.
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