Synthesis, cytotoxicity and antitumor activity of 2,3-diarylcyclopent-2-ene-1-ones

被引：12
|
作者：
Nam, NH
Kim, Y
You, YJ
Hong, DH
Kim, HM
Ahn, BZ [1 ]
机构：
[1] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea
[2] Res Inst Biosci & Biotechnol, Taejon 305600, South Korea
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2002年 / 25卷 / 05期
关键词：
2,3-diarylcyclopent-2-ene-1-ones; cytotoxicity; and antitumor activity;
D O I：
10.1007/BF02976928
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2asimilar to2f) and 3-aryl-2-(3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a-3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).
引用
收藏
页码：600 / 607
页数：8
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