Next Article in Journal
Biochemical and Electrophysiological Characterization of Two Sea Anemone Type 1 Potassium Toxins from a Geographically Distant Population of Bunodosoma caissarum
Previous Article in Journal
Glycosylation of Conotoxins
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
,
1
,
1
,
1
,
1
,
1,* , 2
,
2
 and
2
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
View Full-Text   |   Download PDF [544 KB, uploaded 24 February 2015]   |  

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 (CC BY 3.0).

Supplementary materials

SciFeed

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
RIS
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

[Return to top]
Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert