Synthesis and Biological Evaluation of Novel Cryptophycin Analogs with Modification in the β-Alanine Region

Article abstract of DOI:10.1016/S0960-894X(98)00682-9

Structure modification of the β-alanine region (fragment C) of the potent antimitotic agent cryptophycin was investigated. This includes: (1) introduction of substituents at the previously unsubstituted C7 position of the macrolide ring and (2) replacement of the (2R)-3-amino-2-methyl-propanoic acid (β-alanine) with various (l)-amino acids to give the corresponding 15-membered unnatural cryptophycin analogs.