Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
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.
Varie, David L.,Shih, Chuan,Hay, David A,Andis, Sherri L.,Corbett, Tom H.,Gossett, Lynn S.,Janisse, Samantha K.,Martinelli, Michael J.,Moher, Eric D.,Schultz, Richard M.,Toth, John E.
p. 369 - 374
(2007/10/03)
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