Ru(II)-based complexes with N-(acyl)-N′,N′-(disubstituted)thiourea ligands: Synthesis, characterization, BSA- and DNA-binding studies of new cytotoxic agents against lung and prostate tumour cells

被引：76

作者：

Correa, Rodrigo S. ^{[1
]}

de Oliveira, Katia M. ^{[1
]}

Delolo, Fabio G. ^{[1
]}

Alvarez, Anislay ^{[2
]}

Mocelo, Raul ^{[2
]}

Plutin, Ana M. ^{[2
]}

Cominetti, Marcia R. ^{[3
]}

Castellano, Eduardo E. ^{[4
]}

Batista, Alzir A. ^{[1
]}

机构：

[1] Univ Fed Sao Carlos, Dept Quim, BR-13561901 Sao Carlos, SP, Brazil

[2] Univ La Habana, Fac Quim, Lab Sintesis Organ, Havana 10400, Cuba

[3] Univ Fed Sao Carlos, Dept Gerontol, BR-13561901 Sao Carlos, SP, Brazil

[4] Univ Sao Paulo, Inst Fis Sao Carlos, Dept Fis & Informat, BR-13560970 Sao Carlos, SP, Brazil

来源：

JOURNAL OF INORGANIC BIOCHEMISTRY | 2015年 / 150卷

基金：

巴西圣保罗研究基金会;

关键词：

Ruthenium/phosphine/diimine complexes; Acylthiourea ligands; Prostate cancer; Lung cancer; DNA binding; BSA binding; RUTHENIUM(II) COMPLEXES; MOLECULAR-STRUCTURE; BREAST-CANCER; CRYSTAL; COORDINATION; CONFORMATION; DERIVATIVES; OXYGEN;

D O I：

10.1016/j.jinorgbio.2015.04.008

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：

Four ruthenium(II)-based complexes with N-(acyl)-N',N'-(disubstituted)thiourea derivatives (Th) were obtained. The compounds, with the general formula trans-[Ru(PPh3)(2)(Th)(bipy)]PF6, interact with bovine serum albumin (BSA) and DNA. BSA-binding constants, which were in the range of 3.3-6.5 x 10(4) M-1, and the thermodynamic parameters (Delta G, Delta H and Delta S), suggest spontaneous interactions with this protein by electrostatic forces due to the positive charge of the complexes. Also, binding constant by spectrophotometric DNA titration (Kb = 0.8-1.8 x 10(4) M-1) and viscosity studies indicate weak interactions between the complexes and DNA. Cytotoxicity assays against DU-145 (prostate cancer) and A549 (lung cancer) tumour cells revealed that the complexes are more active in tumour cells than in normal (L929) cells, and that they present high cytotoxicity (low IC50 values) compared with the reference metallodrug, cisplatin. (C) 2015 Published by Elsevier Inc.

引用

页码：63 / 71

页数：9