Li Zhiyu, Zhai Fuming, Zhao Li, Guo Qinglong, You Qidong
Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
Bioorg Med Chem Lett. 2009 Jan 15;19(2):406-9. doi: 10.1016/j.bmcl.2008.11.061. Epub 2008 Nov 21.
A novel series of N-methylmaleimide indolocarbazole derivatives bearing modified 2-acetamino acid moieties are first reported. The cytotoxic effects of these compounds were tested in five human tumor cell lines. The potent compounds 9a, 9b, 9d, and 9e have been further evaluated for their effect on Topoisomerase I (TOPO I) and cancer cell cycle. It is concluded that the indolocarbazoles with alkyl piperazine or morpholine substituent groups instead of esters or glycosyl residues would have better activities against tumors.
首次报道了一系列带有修饰的2-乙酰氨基酸部分的新型N-甲基马来酰亚胺吲哚咔唑衍生物。在五种人类肿瘤细胞系中测试了这些化合物的细胞毒性作用。对强效化合物9a、9b、9d和9e进一步评估了它们对拓扑异构酶I（TOPO I）和癌细胞周期的影响。得出结论，具有烷基哌嗪或吗啉取代基而非酯或糖基残基的吲哚咔唑对肿瘤具有更好的活性。
