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Mar. Drugs 2013, 11(11), 4487-4509; doi:10.3390/md11114487
Article

Derivatives of Salarin A, Salarin C and Tulearin A—Fascaplysinopsis sp. Metabolites

1,†
, 1,†
, 2
, 3
, 3
 and 1,*
1 School of Chemistry, Tel Aviv University, Ramat Aviv 69978, Israel 2 Laboratorie de Chimie des Substances Naturelles et des Aliments, Faculté des Sciences et Techniques, Université de la Réunion, 15 Avenue Rene Cassin, BP 7151, Saint Denis 97715, Cedex 9, France 3 Department of Cell and Developmental Biology, Sackler Faculty of Medicine, Tel Aviv University, Ramat Aviv 69978, Israel These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 30 August 2013 / Revised: 26 September 2013 / Accepted: 9 October 2013 / Published: 11 November 2013
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Abstract

Derivatives of salarin A, salarin C and tulearin A, three new cytotoxic sponge derived nitrogenous macrolides, were prepared and bio-evaluated as inhibitors of K562 leukemia cells. Interesting preliminary SAR (structure activity relationship) information was obtained from the products. The most sensitive functionalities were the 16,17-vinyl epoxide in both salarins, the triacylamino group in salarin A and the oxazole in salarin C (less sensitive). Regioselectivity of reactions was also found for tulearin A.
Keywords: salarins; tulearins; Fascaplysinopsis sp.; sponge; nitrogenous macrolide; leukemia cells salarins; tulearins; Fascaplysinopsis sp.; sponge; nitrogenous macrolide; leukemia cells
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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Zur, L.G.; Bishara, A.; Aknin, M.; Neumann, D.; Ben-Califa, N.; Kashman, Y. Derivatives of Salarin A, Salarin C and Tulearin A—Fascaplysinopsis sp. Metabolites. Mar. Drugs 2013, 11, 4487-4509.

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