Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)

Article abstract of DOI:10.1016/S0960-894X(98)00748-3

Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models.