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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Structure and biological properties of five Pt(II) complexes as potential anticancer agents
Jungang Deng1, Jun Wang1, MuhammadHamid Khan1
1State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Ministry of Science and Technology of China, Guangxi Normal University, Guilin, Guangxi, China.
Abstract:
We synthesized and validated five Schiff base Pt(II) complexes derived from 2-hydroxy-1-naphthaldehyde benzoyl hydrazone and its derivatives, which are modified at the benzohydrazide structures (L1-L5). The complexes were [Pt(L1)(DMSO)Cl] (C1), [Pt(L2)(DMSO)Cl] (C2), [Pt(L3)(DMSO)Cl] (C3), [Pt(L4)(DMSO)Cl] (C4), and [Pt(L5)(DMSO)Cl] (C5). Crystal structures showed that the Pt centers of all complexes were tetra-coordinated with other atoms. The structure-activity relationships and anticancer mechanisms of the complexes were explored. These five Pt(II) complexes were toxic at micromolar doses and exhibited cytotoxicity similar to or somewhat higher than that of cisplatin, with IC50 values ranging from 4.38 μM to 25.16 μM. The complexes exerted chemotherapeutic effects via inhibition of telomerase by targeting the c-myc promoter and down-regulating the expression of human telomerase reverse transcriptase, consequently triggering cell apoptosis. In addition, Pt(II) complexes also caused cell cycle arrest at S-phase, leading to the down-regulation of cdc25 A, cyclin A2, and CDK2 and up-regulation of p53, p27, and p21 proteins. Other complex-associated events were reactive oxygen species production, transformation of the mitochondrial membrane potential (Δψm), release of cytochrome c, regulation of Bcl-2 family protein expression, facilitated release of apoptotic active substances, and activation of caspases to induce apoptosis.
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