Synthesis and preliminary cytotoxicity study of glucuronide derivatives of CC-1065 analogues |
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Authors: | Wang Yuqiang Yuan Huiling Wright Susan C Wang Hong Larrick James W |
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Affiliation: | Panorama Research, Inc., 2462 Wyandotte Street, Mountain View, CA 94043, USA. yuquiangwang@worldnet.att.net |
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Abstract: | Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respectively. Glucuronide 3 is approximately 2-fold less toxic than its hydroxyl counterpart 1, and glucuronide 4 is approximately 6-fold less toxic than its hydroxyl counterpart 2. Glucuronides 3 and 4 may have limited use in the ADEPT approach. However, they may be used as antitumor agents in a conventional way. |
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