CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study

…, W Jiang, H Wang, SC Wright, JW Larrick

Index: Wang, Yuqiang; Li, Lianfa; Ye, Wenqing; Tian, Zhiming; Jiang, Wei; Wang, Hong; Wright, Susan C.; Larrick, James W. Journal of Medicinal Chemistry, 2003 , vol. 46, # 4 p. 634 - 637

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Citation Number: 16

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 ...