Journal of Medicinal Chemistry p. 10512 - 10522 (2012)
Update date:2022-07-30
Topics:
Kurzwernhart, Andrea
Kandioller, Wolfgang
B?chler, Simone
Bartel, Caroline
Martic, Sanela
Buczkowska, Magdalena
Mühlgassner, Gerhard
Jakupec, Michael A.
Kraatz, Heinz-Bernhard
Bednarski, Patrick J.
Arion, Vladimir B.
Marko, Doris
Keppler, Bernhard K.
Hartinger, Christian G.
RuII(arene) complexes have been shown to be promising anticancer agents, capable of overcoming major drawbacks of currently used chemotherapeutics. We have synthesized RuII(η6-arene) compounds carrying bioactive flavonol ligands with the aim to obtain multitargeted anticancer agents. To validate this concept, studies on the mode of action of the complexes were conducted which indicated that they form covalent bonds to DNA, have only minor impact on the cell cycle, but inhibit CDK2 and topoisomerase IIα in vitro. The cytotoxic activity was determined in human cancer cell lines, resulting in very low IC50 values as compared to other RuII(arene) complexes and showing a structure-activity relationship dependent on the substitution pattern of the flavonol ligand. Furthermore, the inhibition of cell growth correlates well with the topoisomerase inhibitory activity. Compared to the flavonol ligands, the RuII(η6-p-cymene) complexes are more potent antiproliferative agents, which can be explained by potential multitargeted properties.
View MoreShifang Taifeng New Flame Retardant Co., Ltd
Contact:02884721008
Address:tingjiang industrial park, hefeng town
Improve Medical Technology(Nanxiong) Co., Ltd
Contact:86-751-3836997
Address:No.33, Pingan First Road, Fine Chemical Industry Base, Nanxiong City, Shaoguan, Guangdong, China
Shanghai Puda Chemical Co.,Ltd
Contact:+86+571+56565965
Address:10F Haiyue Building,Danfeng Road,Binjiang District,Hangzhou,China
Weifang Ocean Trading Co., Ltd.
Contact:+86-536-2081155
Address:Room2606, Yuqing Building, 518#, Yuquan Road, High-tech Development Zone, Weifang City, Shandong Province, China
Henan Yellow River New Material Technology Co.Ltd.
website:http://www.yellowriverchem.com
Contact:0086-373-7278760
Address:Chengguan Town, Yuanyang County
Doi:10.1021/ol303023y
(2012)Doi:10.1055/s-0037-1612087
(2019)Doi:10.1021/ol302842h
(2012)Doi:10.1107/S0108270112038462
(2012)Doi:10.1002/adsc.201200367
(2012)Doi:10.1107/S0108270112017659
(2012)