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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 (CC BY 3.0).

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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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