Journal
DALTON TRANSACTIONS
Volume 40, Issue 34, Pages 8611-8621Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1dt10084j
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Funding
- National Basic Research Program (973 Program) [2007CB815800]
- International S&T Cooperation Program [2007DFA30840]
- State High-Tech Development Program (863 Program) [2006AA090504, 2007AA091401, 2008AA09Z401]
- China Postdoctoral Science Foundation [20080440790]
- Commission of Science and Technology of Guangdong Province and Guangzhou City
- Sun Yet-sen University Science Foundation
- National Natural Science Foundation of China
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Three novel Ru(II) complexes of the general formula [Ru(N-N)(2)(Norharman)(2)](SO3CF3)(2), where N-N = 2,2'-bipyridine (bpy, 1), 1,10-phenanthroline (phen, 2), 4,7-diphenyl-1,10-phenanthroline (DIP, 3) and Norharman (9H-pyrido[3,4-b]indole) is a naturally occurring beta-carboline alkaloid, have been synthesized and characterized. The molecular structures of 1 and 2 have been determined by X-ray diffraction analysis. The cellular uptake efficiencies, in vitro cytotoxicities and apoptosis-inducing properties of these complexes have been extensively explored. Notably, 1-3 exhibit potent antiproliferative activities against a panel of human cancer cell lines with IC50 values lower than those of cisplatin. Further studies show that 1-3 can cause cell cycle arrest in the G0/G1 phase and induce apoptosis through mitochondrial dysfunction and reactive oxygen species (ROS) generation. In vitro DNA binding studies have also been conducted to provide information about the possible mechanism of action.
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