Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

被引：92

作者：

Karki, Radha ^{[3
]}

Thapa, Pritam ^{[3
]}

Kang, Mi Jeong ^{[3
]}

Jeong, Tae Cheon ^{[3
]}

Nam, Jung Min ^{[1
,2
]}

Kim, Hye-Lin ^{[1
,2
]}

Na, Younghwa ^{[4
]}

Cho, Won-Jea ^{[5
]}

Kwon, Youngjoo ^{[1
,2
]}

Lee, Eung-Seok ^{[3
]}

机构：

[1] Ewha Womans Univ, Coll Pharm, Seoul 120750, South Korea

[2] Ewha Womans Univ, Div Life & Pharmaceut Sci, Seoul 120750, South Korea

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

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

[5] Chonnam Natl Univ, Coll Pharm, Kwangju 500757, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 09期

关键词：

Hydroxylated 2,4-diphenyl-6-aryl pyridines; Topoisomerase I and II inhibitor; Cytotoxicity; Anticancer agents; DNA TOPOISOMERASES; CANCER CELLS; DERIVATIVES; COMPLEXES; COVALENT; AGENTS;

D O I：

10.1016/j.bmc.2010.03.051

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group( s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity. (c) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3066 / 3077

页数：12

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