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Bioorg Med Chem Lett. 2011 Jun 1;21(11):3198-201. doi: 10.1016/j.bmcl.2011.04.069. Epub 2011 Apr 24.

Actin depolymerizing effect of trisoxazole-containing macrolides.

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Department of Agricultural Biotechnology, College of Agriculture and Life Science, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-921, Republic of Korea.


Oxazole-containing macrolides (1-5) isolated from the marine sponge Chondrosia corticata were evaluated for their actin depolymerizing activities by monitoring fluorescent intensity of pyrene F-actin. These studies led to the identification of (19Z)-halichondramide (5) as a new actin depolymerizing agent. The actin depolymerizing activity by (19Z)-halichondramide (5) was four times more potent than that of halichondramide (1). Compounds 1 and 5 also have potent antifungal activity. The preliminary structure-activity relationship of these compounds is described to elucidate the essential structural requirements.

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