Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

被引:55
作者
Thapa, Uttam [2 ]
Thapa, Pritam [2 ]
Karki, Radha [2 ]
Yun, Minho [2 ]
Choi, Jae Hun [2 ]
Jahng, Yurngdong [2 ]
Lee, Eunyoung [1 ]
Jeon, Kyung-Hwa [1 ]
Na, Younghwa [3 ]
Ha, Eun-Mi [3 ]
Cho, Won-Jea [4 ]
Kwon, Youngjoo [1 ]
Lee, Eung-Seok [2 ]
机构
[1] Ewha Womans Univ, Coll Pharm, Div Life & Pharmaceut Sci, Seoul 120750, South Korea
[2] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
[3] Catholic Univ Daegu, Coll Pharm, Kyongsan 712702, South Korea
[4] Chonnam Natl Univ, Coll Pharm, Kwangju 500757, South Korea
关键词
Terthiophene; Terpyridine; 4-chromanone; Topoisomerase I and II; Cytotoxicity; 2,4,6-TRISUBSTITUTED PYRIDINE; DNA TOPOISOMERASES; NUCLEASE ACTIVITY; DERIVATIVES; CELLS; COMPLEXES; CHROMENE;
D O I
10.1016/j.ejmech.2011.04.029
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:3201 / 3209
页数:9
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