@article {KHAN2019333, title = {In~vitro and in~vivo anti-tumor activity of two gold(III) complexes with isoquinoline derivatives as ligands}, journal = {Eur. J. Med. Chem.}, volume = {163}, year = {2019}, pages = {333 - 343}, abstract = {

Two gold(III) complexes of isoquinoline derivatives: [Au(L1)Cl2] (Au1) and [Au(L2)Cl2] (Au2) have been prepared and characterized. Au1 and Au2 exhibited greater cytotoxicity than their corresponding ligands and cisplatin against T-24 cells. Both complexes arrested cell cycle at S-phase by upregulation of p53, p27, and p21, and downregulation of cyclin A and cyclin E. The depolarization of the mitochondrial membrane potential, generation of ROS, and stimulated Ca2+ release activated the caspase cascade and ultimately caused apoptosis by increasing the levels of Bax and Bak, and decreasing the levels of Bcl-2 and Bcl-xl. Cell apoptosis was achieved via mitochondria mediated pathways. The in\ vivo studies of Au1 and Au2 demonstrated that they were safer than cisplatin and could effectively inhibit tumor growth.

}, keywords = {ANTITUMOR ACTIVITY, Cell apoptosis, Gold(III) complexes, Isoquinoline, Mitochondrial dysfunction}, issn = {0223-5234}, doi = {https://doi.org/10.1016/j.ejmech.2018.11.047}, url = {http://www.sciencedirect.com/science/article/pii/S0223523418310067}, author = {Taj-Malook Khan and Noor Shad Gul and Xing Lu and Jian-Hua Wei and Yan-Cheng Liu and Hongbin Sun and Hong Liang and Chris Orvig and Zhen-Feng Chen} }