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

…, SL Andis, TH Corbett, LS Gossett, SK Janisse…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 3 p. 369 - 374

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被引用次数: 39

摘要

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.