Song G Y, Kim Y, You Y J, Cho H, Ahn B Z
College of Pharmacy, Chungnam National University, Taejon, Korea.
Arch Pharm Res. 2001 Feb;24(1):35-8. doi: 10.1007/BF02976490.
Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1-hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%
制备了5,8-二甲氧基-1,4-萘醌(DMNQ)的各种类似物,如2-或6-(1-羟基亚氨基烷基)-DMNQ,并对其抗肿瘤作用进行了评估。(1-羟基亚氨基烷基)-DMNQ衍生物比(1-羟烷基)-或酰基-DMNQ衍生物表现出更强的抗肿瘤作用。此外,6-(1-羟基亚氨基烷基)-DMNQ衍生物比2-取代的衍生物表现出更高的抗肿瘤作用,提示存在空间效应。一些具有丁基至辛基部分烷基的6-(1-丙氧基烷基)-DMNQ衍生物的T/C值>400%