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CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity
Yuqiang Wang1, Lianfa Li, Wenqing Ye
1Panorama Research, Inc., 2462 Wyandotte Street, Mountain View, California 94043, USA. yuqiang.wang@worldnet.att.net
Journal of Medicinal Chemistry
|February 7, 2003
Abstract:
CC-1065 analogues bearing different DNA-binding subunits were synthesized. A terminal C5-NO2 and -F moiety at the DNA-binding subunit increased the drug's potency and antitumor efficacy. A C5-OCH3 reduced the potency and antitumor efficacy. Compound (+/-)-7, bearing a trans double bond, had increased antitumor efficacy. A preliminary toxicity study indicated that terminal C5-OCH3 and -acetamido moieties at the DNA-binding subunit caused delayed death in mice.