Synthesis, characterisation and biological activity of the ruthenium(II) complexes of the N4-tetradentate (N4-TL), 1,6-di (2′-pyridyl)-2,5-dibenzyl-2,5-diazahexane (picenBz2)

被引:1
作者
Bjelosevic, Aleksandra [1 ]
Sakoff, Jennette [2 ]
Gilbert, Jayne [2 ]
Zhang, Yingjie [3 ]
McGhie, Brondwyn [1 ]
Gordon, Christopher [1 ]
Aldrich-Wright, Janice R. [1 ,4 ]
机构
[1] Western Sydney Univ, Sch Sci, Locked Bag 1797, Penrith, NSW 2751, Australia
[2] Calvary Mater Newcastle Hosp, Waratah, NSW 2298, Australia
[3] Australian Nucl Sci & Technol Org, Locked Bag 2001, Kirrawee Dc, NSW 2232, Australia
[4] Western Sydney Univ, Sch Med, Locked Bag 1797, Penrith, NSW 2751, Australia
关键词
Ruthenium; N-4-tetradentate; Cell growth inhibition; CHIRAL METAL-COMPLEXES; DNA-BINDING; ORGANOMETALLIC CHEMISTRY; CRYSTAL-STRUCTURE; ANTICANCER AGENT; ARENE COMPLEXES; DRUG; CYTOTOXICITY; BEARING; KP1019;
D O I
10.1016/j.jinorgbio.2021.111629
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
A series of complexes of the type rac-cis-beta-[Ru(N-4-TL)(N-2-bidentates)](2+) (where N-4-TL = 1,6-di(2'-pyridyl)-2,5-dibenzyl-2,5-diazahexane (picenBz(2), N-4-T-L-2) and N-2-bidentates = 1,10-phenanthroline (phen, Ru-2), dipyrido [3,2-d:2',3'[-f]quinoxaline (dpq, Ru-3), 7,8-dimethyl-dipyrido[3,2-a:2;,3'-c] phenazine (dppzMe2, Ru-4), 2phenyl-1H-imidazo[4,5-f][1,10]phenanthroline (phenpyrBz, Ru-5), 2-(p-tolyl)-1H-imidazo[4,5-f][1,10]phenan-throline (phenpyrBzMe, Ru-6), 2-(4-nitrophenyl)-1H-imidazo[4,5-f][1,10]phenanthroline (phenpyrBzNO(2), Ru7), were synthesised and characterised and X-ray crystallography of Ru-5 obtained. The in vitro cytotoxicity assays revealed that Ru-6 was 5, 2 and 19-fold more potent than oxaliplatin, cisplatin, and carboplatin, respectively displaying an average GI(50) value of approximate to 0.76 mu M against a panel of 11 cancer cell lines.
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页数:11
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