作者
Alexander L Ruchelman, Sudhir K Singh, Xiaohua Wu, Abhijit Ray, Jin-Ming Yang, Tsai-Kun Li, Angela Liu, Leroy F Liu, Edmond J LaVoie
发表日期
2002/11/18
期刊
Bioorganic & medicinal chemistry letters
卷号
12
期号
22
页码范围
3333-3336
出版商
Pergamon
简介
Several 5,12-diazachrysen-6-ones and 5,6,11-triazachrysen-12-ones were synthesized with varied substituents at the 5- or 11-position, respectively. Each compound was evaluated for its potential to stabilize the cleavable complex formed with TOP1 and DNA. Two analogues with very potent TOP1-targeting activity, 3a and 4a, exhibited cytotoxic activity with IC50 values at or below 2nM against RPMI8402. Compound 3a was active in vivo by either ip or po administration in the human tumor xenograft athymic nude mice model.
引用总数
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AL Ruchelman, SK Singh, X Wu, A Ray, JM Yang, TK Li… - Bioorganic & medicinal chemistry letters, 2002