2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

被引：127

作者：

Basnet, Arjun

Thapa, Pritam

Karki, Radha

Na, Younghwa

Jahng, Yurngdong

Jeong, Byeong-Seon

Jeong, Tae Cheon

Lee, Chong-Soon

Lee, Eung-Seok ^{[1
]}

机构：

[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea

[2] Catholic Univ Daegu, Coll Pharm, Kyongsan 712702, South Korea

[3] Yeungnam Univ, Dept Biochem, Kyongsan 712749, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 13期

基金：

新加坡国家研究基金会;

关键词：

2,4,6-trisubstituted pyridines; topoisomerase I and II; cytotoxicity; antitumor agent;

D O I：

10.1016/j.bmc.2007.04.047

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10-20 showed significant topoisomerase I or II inhibitory activities, and 21-26 showed considerable cytotoxicities against several human cancer cell lines. Structure-activity relationship study indicates that 4-pyridine at 6-position of central pyridine plays a key role in biological activity. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4351 / 4359

页数：9

共 19 条

[1]

Oxidation of DNA and RNA by oxoruthenium(IV) metallointercalators: Visualizing the recognition properties of dipyridophenazine by high-resolution electrophoresis [J].