Synthesis, characterization and antitumor activity of novel gold (III) compounds with cisplatin-like structure

摘要

Gold(III) centers are isoelectronic to Pt(II) compounds and adopt square-planar configurations similar to that of cisplatin, gold (III) compounds could display strong effects of tumor cell growth inhibition by a non-cisplatin-like mode of action. In our present work, we synthesized and characterized three gold(III) complexes which are coordinated by the N atom of amide group and investigated their in vitro anticancer activity, including their mechanism of action. In screening their in vitro activity, we found three gold complexes to exhibit selectivity of cytotoxicity, and complex 3 display better anticancer activity than another two gold(III) compounds and cisplatin. The three gold (III) complexes show preference to accumulation in mitochondria. The complex 3 could inhibit the growth of tumor cell by inducing the apoptosis mediated by ER-stress through loss of cellular homeostasis disrupts Ca2+ signaling. Based on our results, we believe complex 3 to be a promising anticancer agent or lead compound for further anticancer drug development.