Derivatives of salarin A, salarin C and tulearin A--Fascaplysinopsis sp. metabolites.

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.

• Authors: Lee Goren Zur, Ashgan Bishara, Maurice Aknin, Drorit Neumann, Nathalie Ben-Califa, Yoel Kashman
• Journal: Marine drugs (Mar Drugs) Vol. 11 Issue 11 Pg. 4487-509 (Nov 11 2013) ISSN: 1660-3397 [Electronic] Switzerland
• PMID: 24284425 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Macrolides
• salarin A
• salarin C
• tulearin

Topics

• Animals
• Cell Line, Tumor
• Humans
• K562 Cells
• Macrolides (chemistry, pharmacology)
• Porifera (chemistry)
• Structure-Activity Relationship