Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors

被引：18

作者：

Khadka, Daulat Bikram ^{[1
,2
]}

Quynh Manh Le ^{[1
,2
]}

Yang, Su Hui ^{[1
,2
]}

Hue Thi My Van ^{[1
,2
]}

Thanh Nguyen Le ^{[1
,2
]}

Cho, Suk Hee ^{[1
,2
]}

Kwon, Youngjoo ^{[3
]}

Lee, Kyung-Tae ^{[4
]}

Lee, Eung-Seok ^{[5
]}

Cho, Won-Jea ^{[1
,2
]}

机构：

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

[2] Chonnam Natl Univ, Res Inst Drug Dev, Kwangju 500757, South Korea

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

[4] Kyung Hee Univ, Coll Pharm, Seoul 130701, South Korea

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 06期

关键词：

Indeno[1,2-c]isoquinolines; Topoisomerase I; Cytotoxicity; Docking study; DRUG CAMPTOTHECIN; CYTOTOXICITY; 3-ARYLISOQUINOLINES; AGENTS; RING;

D O I：

10.1016/j.bmc.2011.01.064

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：

Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1924 / 1929

页数：6

共 17 条

[1]

ARNOULD R, 1990, ANTICANCER RES, V10, P145

[2]

BJORNSTI MA, 1989, CANCER RES, V49, P6318

[3] Synthesis of new 3-arylisoquinolinamines: Effect on topoisomerase I inhibition and cytotoxicity [J].