新型吲哚基嘧啶和吲哚基吡嗪作为潜在抗肿瘤药物的合成及细胞毒性评价
Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents.
作者信息
Jiang B, Yang C G, Xiong W N, Wang J
机构信息
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, P. R., Shanghai 200032, China.
出版信息
Bioorg Med Chem. 2001 May;9(5):1149-54. doi: 10.1016/s0968-0896(00)00337-0.
Novel indolylpyrimidines and indolylpyrazines have been synthesized as potential antitumor agents. They were screened in a panel of 60 human tumor cell lines in vitro. Compounds 7, 9, 10, 15, 21 exhibited efficiently cytotoxic activities with GI(50) values in the low micromolar range against a variety of human cancer cell lines. 2,4-Bis(3'-indolyl)pyrimidine 8 displayed selective cytotoxic activity against IGROV1 tumor cell line with the GI(50) value below 0.01 microM.
新型吲哚基嘧啶和吲哚基吡嗪已被合成为潜在的抗肿瘤药物。它们在60种人类肿瘤细胞系的体外实验中进行了筛选。化合物7、9、10、15、21对多种人类癌细胞系表现出高效的细胞毒性活性，其GI(50)值在低微摩尔范围内。2,4-双(3'-吲哚基)嘧啶8对IGROV1肿瘤细胞系表现出选择性细胞毒性活性，其GI(50)值低于0.01微摩尔。
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