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Updated: Mar 12, 2026
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Mechanistic Studies of the Anticancer Activity of An Octahedral Hexanuclear Pt(II) Cage
Yao-Rong Zheng1, Kogularamanan Suntharalingam1, Peter M Bruno2
1Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139.
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.
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