Synthesis, spectral characterization, DNA binding ability and anti-cancer screening of new acridine-based derivatives

被引:12
|
作者
Salem, Othman M. [1 ]
Vilkova, Maria [2 ]
Janockova, Jana [1 ,3 ]
Jendzelovsky, Rastislav [4 ]
Fedorocko, Peter [4 ]
Imrich, Jan [2 ]
Kozurkova, Maria [1 ,3 ]
机构
[1] Safarik Univ, Dept Biochem, Kosice, Slovakia
[2] Safarik Univ, Inst Chem, Dept Organ Chem, Kosice, Slovakia
[3] Univ Hosp Hradec Kralove, Biomed Res Ctr, Hradec Kralove, Czech Republic
[4] Safarik Univ, Inst Biol & Ecol, Dept Cellular Biol, Fac Sci, Kosice, Slovakia
关键词
Acridine derivatives; Topoisomerases I and II; HL-60; cells; DNA binding; TOPOISOMERASE-I; ANTITUMOR-ACTIVITY; LINEAR DICHROISM; ACID; INHIBITION; COMPLEXES; ESTERIFICATION; THIAZACRIDINE; APOPTOSIS; AGENTS;
D O I
10.1007/s00044-017-1931-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, a series of newly synthesized acridine derivatives, compounds 4, 6a, and 6b, are described and their biological activity on HL-60 cell lines is assessed using a number of different techniques. Binding studies were also performed between the derivatives and DNA in order to characterize the mechanism of the agents' effect in more detail. The results of ultraviolet-visible absorption spectroscopy prove that the binding of derivatives 4, 6a, and 6b had occurred with a binding constant value of K = 3.5 x 10(4)-4.0 x 10(4) M-1. These findings are indicative of a strong interaction between the derivatives and DNA, and this hypothesis is supported by the results of the fluorescence emission, linear dichroism, and viscometric assays.
引用
收藏
页码:2309 / 2321
页数:13
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