吲哚试验
化学
K562细胞
立体化学
慢性粒细胞白血病
癌细胞系
白血病
结构-活动关系
组合化学
细胞培养
计算生物学
癌细胞
生物化学
癌症
细胞
体外
免疫学
生物
遗传学
作者
Romeo Romagnoli,Pier Giovanni Baraldi,María Dora Carrión,Olga Cruz‐López,Carlota Lopez Cara,Delia Preti,Mojgan Aghazadeh Tabrizi,Jan Balzarini,Ernest Hamel,Enrica Fabbri,Roberto Gambari
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2009-06-01
卷期号:6 (4): 298-303
被引量:15
标识
DOI:10.2174/157018009788452519
摘要
Identification of novel and selective anticancer agents remains an important and challenging goal in pharmacological research. The indole nucleus, frequently encountered as a molecular fragment in natural products and pharmaceutically active compounds, was employed as the initial building block for the synthesis of a series of pyrazino[1,2-a]indoles 1a-k, variably substituted at the 6, 7, 8 and 9-positions. Compound 1e, bearing the methoxy group at the 8-position of the pyrazino[1,2-a]indole nucleus was identified as a novel potent antiproliferative agent against the human chronic myelogenous leukemia K562 cell line, but it was much less active against several other cancer cell lines. Comparison of positional isomers indicated that moving the methoxy group from the 8- to the 7- or 6-position, to furnish compounds 1f and 1g, respectively, yielded inactive compounds. The analysis of structure-activity relationships observed in the series of investigated compounds may represent the basis for the design of more active molecules.
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