Gelastatin A and B, isolated from culture broth of Westerdykella multispora F 50733, have been reported to exhibit MMP-inhibitory activities at a sub-micromolar level. In an effort to exploit this lead, we synthesized gelastatin analogues in which the conjugated triene unit of natural gelastatins was replaced by the benzylidene group. The (Z)-isomeric synthetic benzylidene-gelastatin exhibited MMP-inhibitory activities comparable to those reported for the natural products. Therefore, this compound appears to be a viable lead in searching for therapeutically useful MMP inhibitors.
|Number of pages||6|
|Journal||Helvetica Chimica Acta|
|State||Published - 2002|