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Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region
C Shih1, L S Gossett, J M Gruber
1Lilly Research Laboratories, Indianapolis, IN 46285, USA.
Bioorganic & Medicinal Chemistry Letters
|February 17, 1999
Abstract:
Structure modification of the beta-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 (beta-alanine) with various (1)-amino acids to give the corresponding 15-membered unnatural cryptophycin analogs.