Author/Authors :
David L. Varie، نويسنده , , Chuan Shih، نويسنده , , David A. Hay، نويسنده , , Sherri L. Andis، نويسنده , , Tom H. Corbett، نويسنده , , Lynn S. Gossett، نويسنده , , Samantha K. Janisse، نويسنده , , Michael J. Martinelli، نويسنده , , Eric D. Moher، نويسنده , , Richard M. Schultz، نويسنده , , John E. Toth، نويسنده ,
Abstract :
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.