Mechanistic Studies of the Anticancer Activity of An Octahedral Hexanuclear Pt(II) Cage.

Abstract

The cellular response evoked by a hexanuclear platinum complex, Pt6L4 (1), is reported. Compound 1, a 3-nm octahedral cage formed by self-assembly of six Pt(II) centers and four 2,4,6-tris(4-pyridyl)-1,3,5-triazine ligands (L), exhibits promising in vitro potency against a panel of human cancer cell lines. Unlike classical platinum-based anticancer agents, 1 interacts with DNA in a non-covalent, intercalative manner and promotes DNA condensation. In cancer cells, 1 induces DNA damage, upregulates p53, its phosphorylated form phospho-p53 and its downstream effector, p21, as well as both apoptosis and senescence.

• Authors: Yao-Rong Zheng, Kogularamanan Suntharalingam, Peter M Bruno, Wei Lin, Weixue Wang, Michael T Hemann, Stephen J Lippard
• Journal: Inorganica chimica acta (Inorganica Chim Acta) Vol. 452 Pg. 125-129 (Oct 01 2016) ISSN: 0020-1693 [Print] Switzerland
• PMID: 27818526 (Publication Type: Journal Article)