Anticancer evaluation of ruthenium(III) complexes with N-donor ligands tethered to coumarin or uracil moieties

被引：24

作者：

Gramni, Larusha ^{[1
]}

Vukea, Nyeleti ^{[2
]}

Chakraborty, Abir ^{[2
]}

Samson, William John ^{[2
]}

Dingle, Laura Margaret Kirkpartick ^{[2
]}

Xulu, Bheki ^{[1
]}

de la Mare, Jo-Anne ^{[2
]}

Edkins, Adrienne Lesley ^{[2
]}

Booysen, Irvin Noel ^{[1
]}

机构：

[1] Univ KwaZulu Natal, Sch Chem & Phys, Pietermaritzburg, South Africa

[2] Rhodes Univ, Biomed Biotechnol Res Unit, Dept Biochem & Microbiol, Grahamstown, South Africa

来源：

INORGANICA CHIMICA ACTA | 2019年 / 492卷 / 98-107期

基金：

新加坡国家研究基金会;

关键词：

Ruthenium; Dipicolyamine; Chromone; Uracil; DNA interactions; Cytotoxicity; DNA-BINDING; SUBSTITUTION-REACTIONS; ANTITUMOR-ACTIVITY; CANCER CELLS; IN-VITRO; CYTOTOXICITY; ACTIVATION; KINETICS; DOCKING; OSMIUM;

D O I：

10.1016/j.ica.2019.04.018

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

In this study, the synthesis and characterization of new paramagnetic ruthenium(III) complexes: cis-[RuCl2(urdpa)] (1) {Hurdpa = 6-((bis(pyridin-2-ylmethyl)amino)methyl)uracil} and fac-[RuCl3(chrdpa)] (2) {chrdpa = 4-((bis(pyridin-2-ylmethyl)amino)methyl)-7-methoxycoumarin} are reported. These metal complexes have been comprehensively characterized by an array of physicochemical techniques and the X-ray solid-state structures of 1 and Hurdpa have been attained. Electronic spectroscopy Calf-Thymus DNA titrations revealed that both 1 and 2 are groove binders while molecular docking calculations indicated that the ligands' steric factors dictate the mode of interaction of these individual ruthenium(III) species. These mononuclear ruthenium compounds were screened against cervical and breast cancer cell lines and show activity in the high micromolar range.

引用

页码：98 / 107

页数：10

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