Bioorganic & Medicinal Chemistry 2007-08-01

Antiangiogenic versus cytotoxic activity in analogues of aeroplysinin-1.

Rubén Córdoba, Nélida Salvador Tormo, Antonio Fernández Medarde, Joaquín Plumet

Index: Bioorg. Med. Chem. 15 , 5300-15, (2007)

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Abstract

A series of analogues of the potentially angiogenic inhibitor aeroplysinin-1 1 were synthesized and their in vitro antiangiogenic and cytotoxic activities evaluated. In the case of epoxy ketone 6 and azlactone 36 the relationship sprouting inhibition assay/cytotoxicity in BAE cells was enhanced by one order and two orders of magnitude, respectively, with respect to the reference. These results imply more specific antiangiogenic properties for the synthesized derivatives.

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