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Mar. Drugs 2015, 13(1), 655-665; doi:10.3390/md13010655

Design, Synthesis and Evaluation of New Marine Alkaloid-Derived Pentacyclic Structures with Anti-Tumoral Potency

1
Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Decatur, GA 30033, USA
2
University François Rabelais de Tours, EA2106 Biomolécules et Biotechnologies Végétales, 31 avenue Monge, 37200 Tours, France
3
University of Poitiers, UMR CNRS IC2MP 7285, 40 avenue du Recteur Pineau, 86022 Poitiers Cedex, France
*
Author to whom correspondence should be addressed.
Academic Editor: Yoshihide Usami
Received: 4 November 2014 / Revised: 10 December 2014 / Accepted: 9 January 2015 / Published: 19 January 2015
(This article belongs to the Special Issue Synthesis around Marine Natural Products)
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Abstract

This work describes the synthesis and biological evaluation of a new heterocyclic hybrid derived from the ellipticine and the marine alkaloid makaluvamine A. Pyridoquinoxalinedione 12 was obtained in seven steps with 6.5% overall yield. 12 and its intermediates 111 were evaluated for their in vitro cytotoxic activity against different cancer cell lines and tested for their inhibitory activity against the human DNA topoisomerase II. The analysis by electrophoresis shows that the pentacycle 12 inhibits the topoisomerase II like doxorubicine at 100 µM. Compound 9 was found to have an interesting profile, having a cytotoxicity of 15, 15, 15 and 10 μM against Caco-2, HCT-116, Pc-3 and NCI cell lines respectively, without any noticeable toxicity against human fibroblast. View Full-Text
Keywords: makaluvamine; pyrroloiminoquinone; marine drugs analogues; topoisomerase II inhibitor; antitumor activity makaluvamine; pyrroloiminoquinone; marine drugs analogues; topoisomerase II inhibitor; antitumor activity
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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. (CC BY 4.0).

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MDPI and ACS Style

Boucle, S.; Melin, C.; Clastre, M.; Guillard, J. Design, Synthesis and Evaluation of New Marine Alkaloid-Derived Pentacyclic Structures with Anti-Tumoral Potency. Mar. Drugs 2015, 13, 655-665.

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