This invention is directed to didemnin derivatives, including N-acyl congeners of didemnin A (DA); several DDB-type analogues of DA in which either pyruvic acid has been replaced (with phenylpyruvic acid or alphaketobutyric acid) or proline at position 8 has been replaced [with L-azetidine-2-carboxylic acid (AZT), L-pipecolic acid (Pip), 1-amino-1-carboxylic cyclopentane (acc.sup.5), D-Pro or sarcosine (sar); and other cyclic depsipeptides related to the didemnins, which were isolated from a relatively polar extract of the tunicate T. solidum; namely the didemnins--X [(R)-3-hydroxy-decanoyl-(Gln).sub.3 -Lac-Pro didemnin A]; Y [(R)-3-hydroxy-decanoyl-(Gln).sub.4 -Lac-Pro didemnin A]; M (pGlu-Gln-Lac-Pro-didemnin A); N ([Tyr.sup.5 ] didemnin B); nordidemnin N ([Tyr.sup.5 ] nordidemnin B); and epididemnin A ([2S,4R-Hip.sup.2 ] didemnin A).
|Original language||English (US)|
|U.S. patent number||5294603|
|State||Published - Mar 15 1994|