Derivatives of dehydrodidemnin B

Abstract

Dehydrodidemnin with useful biological activity has formula (1). It can be isolated from natural sources or synthesized, and it forms active derivatives.

What is claimed is:  
     
         1 . The substantially pure compound, Dehydrodidemnin B, essentially free of the cellular debris of the Mediterranean tunicate,  Aplidium albicans , said compound having the formula:  
       
         
           
           
               
               
           
         
       
     
     
         2 . An acylated, alkylated or arylated derivative of dehydrodidemnin B wherein the acyl, alkyl, or aryl groups are selected from C 1  to C 6  alkyl, C 1  to C 6  acyl, phenyl, benzyl, or C 1  to C 6  alkylphenyl.  
     
     
         3 . A pharmaceutical composition which comprises dehydrodidemnin B or an active acylated, alkylated or arylated derivative thereof, together with a pharmaceutically acceptable carrier, wherein the acyl, alkyl, or aryl groups are selected from either C 1  to C 6  alkyl, C 1  to C 6  acyl, phenyl, benzyl, or C 1  to C 6  alkylphenyl.  
     
     
         4 . A semisynthetic process for the preparation of dehydrodidemnin B, which comprises the coupling of pyruvyl-proline to didemnin A.  
     
     
         5 . A method for isolation of dehydrodidemnin B which comprises extraction from a dehydrodidemnin B-containing tunicate.  
     
     
         6 . The monoacetyl derivative of dehydrodidemnin B.