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
收藏
页码：3066 / 3077
页数：12
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