Abstract
A series of arene Ru(II) complexes coordinated with phenanthroimidazole derivatives, [(η6-C6H6)Ru(l)Cl]Cl(1b L = p-ClPIP = 2-(4-Chlorophenyl)imidazole[4,5f] 1,10-phenanthroline; 2b L = m-ClPIP = 2-(3-Chlorophenyl)imidazole[4,5f] 1,10-phenanthroline; 3b L = p-NPIP = 2-(4-Nitrophenyl)imidazole[4,5f] 1,10-phenanthroline; 4b L = m-NPIP = 2-(3-Nitrophenyl) imidazole [4,5f] 1,10-phenanthroline) were synthesized in yields of 89.9%–92.7% under conditions of microwave irradiation heating for 30 min to liberate four arene Ru(II) complexes (1b, 2b, 3b, 4b). The anti-tumor activity of 1b against various tumor cells was evaluated by MTT assay. The results indicated that this complex blocked the growth of human lung adenocarcinoma A549 cells with an IC50 of 16.59 μM. Flow cytometric analysis showed that apoptosis of A549 cells was observed following treatment with 1b. Furthermore, the in vitro DNA-binding behaviors that were confirmed by spectroscopy indicated that 1b could selectively bind and stabilize bcl-2 G-quadruplex DNA to induce apoptosis of A549 cells. Therefore, the synthesized 1b has impressive bcl-2 G-quadruplex DNA-binding and stabilizing activities with potential applications in cancer chemotherapy.
Highlights
Arene Ru(II) complexes have long been considered one of the most promising candidates for anti-cancer drug therapy due in part to their low toxicity and remarkable anti-cancer activity [1].Numerous arene Ru(II) complexes have been designed, and their anti-tumor activity and DNA binding behavior, as well as their underlying mechanisms of action, have been extensively investigated.it was shown that arene Ru(II) complexes can bind and disturb the replication of DNA, and induce apoptosis and tumor cell cycle arrest [2,3,4,5,6,7,8]
It has been determined that arene Ru(II) complexes coordinated with phenanthroimidazole derivatives like [(η6 -C6 H6 )Ru(H2 iip)Cl]Cl (RAWQ11) could effectively inhibit the migration and invasion of breast cancer cells
Four arene RuII complexes were synthesized in a time period of 30 min using microwave-assisted technology, under conditions of rapid rising to the required reaction microwave-assisted technology, under conditions of rapid rising to the required reaction temperature temperature (
Summary
Arene Ru(II) complexes have long been considered one of the most promising candidates for anti-cancer drug therapy due in part to their low toxicity and remarkable anti-cancer activity [1]. Our research group has shown that arene Ru(II) complexes coordinated with phenanthroimidazole exhibit great anti-tumor activity and low toxicity to normal cells, owing to their ability to bind and stabilize the G-quadruplex structure of c-myc and subsequent blocking of the replication of c-myc oligomer [24]. This finding might suggest that arene Ru(II) complexes show stronger binding affinity to bcl-2 G-quadruplex DNA than to duplex DNA (calf thymus DNA).
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