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2-亚苄基环己酮和2,6-双(亚苄基)环己酮的抗肿瘤和细胞毒性活性以及作为酵母线粒体功能抑制剂的评估:(E)-2-亚苄基环己酮的代谢研究

Evaluation of 2-benzylidenecyclohexanones and 2,6-bis(benzylidene)cyclohexanones for antitumor and cytotoxic activity and as inhibitors of mitochondrial function in yeast: metabolism studies of (E)-2-benzylidenecyclohexanone.

作者信息

Dimmock J R, Hamon N W, Hindmarsh K W, Sellar A P, Turner W A, Rank G H, Robertson A J

出版信息

J Pharm Sci. 1976 Apr;65(4):538-43. doi: 10.1002/jps.2600650415.

DOI:10.1002/jps.2600650415
PMID:775053
Abstract

Some 2-benzylidenecyclohexanones, 2,6-bis(benzylidene)cyclohexanones, and related compounds were evaluated for antitumor and cytotoxic activities; (E)-2-benzylidenecyclohexanone (Ia) was shown to have significant cytotoxic properties and a potent inhibitory effect on yeast mitochondria. After intraperitoneal injection of Ia, unchanged drug and a metabolite, tentatively identified as 2-(p-hydroxybenzyl)cyclohexanol, were found in the urine. No metabolites were found in the feces. Oral administration of Ia afforded three unidentified metabolites in the urine and three unidentified metabolites in the feces.

摘要

对一些2-亚苄基环己酮、2,6-双(亚苄基)环己酮及相关化合物进行了抗肿瘤和细胞毒性活性评估;结果表明,(E)-2-亚苄基环己酮(Ia)具有显著的细胞毒性特性,对酵母线粒体有强效抑制作用。腹腔注射Ia后,在尿液中发现了未变化的药物和一种初步鉴定为2-(对羟基苄基)环己醇的代谢物。粪便中未发现代谢物。口服Ia后,尿液中有三种未鉴定的代谢物,粪便中有三种未鉴定的代谢物。

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