氟化苯并噻唑取代的羟基环己-2,5-二烯酮（“喹诺酮”）的抗肿瘤特性
Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols').
作者信息
Lion Cedric J, Matthews Charles S, Wells Geoffrey, Bradshaw Tracey D, Stevens Malcolm F G, Westwell Andrew D
机构信息
Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, UK.
出版信息
Bioorg Med Chem Lett. 2006 Oct 1;16(19):5005-8. doi: 10.1016/j.bmcl.2006.07.072.
The synthesis and in vitro antitumour evaluation of a new series of fluorinated benzothiazole-substituted 4-hydroxycyclohexa-2,5-dienones ('quinols') is described. The new compounds were found to be of comparable activity compared to the non-fluorinated precursor PMX 464, in terms of antiproliferative activity in sensitive human cancer cell lines (nanomolar GI(50) values) and inhibitory activity against the thioredoxin signalling system.
描述了一系列新型氟化苯并噻唑取代的4-羟基环己-2,5-二烯酮（“喹醇”）的合成及其体外抗肿瘤评估。在敏感人类癌细胞系中的抗增殖活性（纳摩尔级的GI(50)值）以及对硫氧还蛋白信号系统的抑制活性方面，发现这些新化合物与未氟化的前体PMX 464具有相当的活性。
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