CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study.
CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study.
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带有不同 DNA 结合亚基的 CC-1065 类似物：合成、抗肿瘤活性和初步毒性研究。
DOI：
10.1021/jm0203433
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发表时间：
2003
期刊：
影响因子：
--
通讯作者：
Larrick,JamesW
中科院分区：
文献类型：
--
作者：
Wang,Yuqiang;Li,Lianfa;Ye,Wenqing;Tian,Zhiming;Jiang,Wei;Wang,Hong;Wright,SusanC;Larrick,JamesW
合成了具有不同DNA结合亚基的CC-1065类似物。DNA结合亚基的末端C5− NO2和−F部分增加了药物的效力和抗肿瘤功效。C5− OCH 3降低了效力和抗肿瘤功效。化合物（±）-7具有较强的抗肿瘤活性。一项初步的毒性研究表明，DNA结合亚基的末端C5− OCH 3和−乙酰氨基部分导致小鼠延迟死亡。
CC-1065 analogues bearing different DNA-binding subunits were synthesized. A terminal C5−NO2and −F moiety at the DNA-binding subunit increased the drug's potency and antitumor efficacy. A C5−OCH3reduced the potency and antitumor efficacy. Compound (±)-7, bearing a trans double bond, had increased antitumor efficacy. A preliminary toxicity study indicated that terminal C5−OCH3and −acetamido moieties at the DNA-binding subunit caused delayed death in mice.