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黄酮 - 8 - 乙酸(FAA)新衍生物的合成与抗肿瘤活性。第1部分:6 - 甲基衍生物。

Synthesis and antitumour activity of new derivatives of flavone-8-acetic acid (FAA). Part 1: 6-Methyl derivatives.

作者信息

Aitken R A, Bibby M C, Double J A, Phillips R M, Sharma S K

机构信息

School of Chemistry, University of St. Andrews, Fife, UK.

出版信息

Arch Pharm (Weinheim). 1996 Nov;329(11):489-97. doi: 10.1002/ardp.19963291104.

Abstract

A range of 17 derivatives of flavone-8-acetic acid (FAA) with a 6-methyl substituent have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. While many of the compounds show activity comparable to FAA in vitro, this essentially disappears in vivo, possibly due to degradation before the compounds can reach the tumour site.

摘要

已制备了一系列具有6-甲基取代基的黄酮-8-乙酸(FAA)衍生物,并在体外针对一组人和小鼠肿瘤细胞系以及在体内针对MAC 15A评估了它们的抗肿瘤活性。虽然许多化合物在体外显示出与FAA相当的活性,但这种活性在体内基本消失,可能是由于化合物在到达肿瘤部位之前就已降解。

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