On the stability and biological behavior of cyclometallated Pt(IV) complexes with halido and aryl ligands in the axial positions

摘要: Abstract A series of cyclometallated platinum(IV) compounds ( 3a , 3a′ and 3b′ ) with a meridional [C,N,N′] terdentate ligand, featuring an halido aryl group in the axial positions has been evaluated for electrochemical reduction preliminary biological behavior against panel human adenocarcinoma (A-549 lung, HCT-116 colon, MCF-7 breast) cell lines normal bronquial epithelial BEAS-2B cells. Cathodic potentials (shifting from −1.463 to −1.570 V) reveal that under study would be highly reluctant reduced environment. Actually ascorbic acid was not able reduce complex most prone according its potential, over period one week. These results suggest intrinsic activity investigated complexes ), which exhibit remarkable cytotoxicity effectiveness (with IC 50 values low micromolar range), even greater than cisplatin. The A-549 lung cells clog P were found follow same trend:  >  . However, no correlation observed between potential vitro activity. As representative example, compound exercise antiproliferative directly non-microcytic cancer through mixture cycle arrest (13% at G1 phase 46% G2 phase) apoptosis induction (increase early by 30 times regard control). To gain further insights into mode action complexes, drug uptake, cathepsin B inhibition ROS generation also evaluated. Interestingly increased could related cisplatin-resistant lines.