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

Mar Drugs. 2013 Nov 11;11(11):4487-509. doi: 10.3390/md11114487.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Macrolides
  • salarin A
  • salarin C
  • tulearin