Bastadins, cyclic tetramers of brominated-tyrosine derivatives, selectively inhibit the proliferation of endothelial cells
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Eight bastadins, tetramers of brominated-tyrosine derivatives, were isolated from the marine sponge Ianthella basta, and their anti-proliferative activities against endothelial cells were examined. A structure-activity relationship study of these compounds revealed that a macrocyclic structure was crucial, and a bastarane-type skeleton was important for the selective activity of these bastadins against endothelial cells. A conformational analysis of the bastadins was also carried out by molecular mechanics calculation.
KeywordsAnti-proliferation Bastadins Endothelial cell Marine sponge
The authors are grateful to the Takeda Science Foundation and the Ministry of Education, Culture, Sports, Science, and Technology of Japan for financial support.
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