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

页码：600 / 607

页数：8

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