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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
Published on: November 10, 2013
Synthesis and anticancer activity of two highly water-soluble and ionic Pt(iv) complexes as prodrugs for Pt(ii)
Anli Gao1, Yaxi Wu2,3, Juan Yu1
1State Key Lab of Advanced Technologies for PGM, Kunming Institute of Precious Metals 988 Keji Road Kunming City 650106 China liuweiping0917@126.com.
Abstract:
Two new Pt(iv) complexes featuring mesylate as the outer sphere anion, cis,trans,cis-[PtCl2(OH2)2(NH3)2](CH3SO3)2 (SPt-1) and cis,trans,cis-[PtCl2(OH2)2(1R,2R-DACH)](CH3SO3)2 (SPt-2), were synthesized and characterized by elemental analysis, 1H and 13C NMR, IR, and ESI-MS. Both complexes have excellent water-solubility, high molar conductivity and good water stability. They exhibit an irreversible two-electron reduction event with the peak potentials (E p) for the processes being -0.40 V for SPt-1 and -0.52 V for SPt-2. The biological tests reveal that SPt-2 possesses high in vitro anticancer activity against three human cancer cell lines (HCT-116, A549 and MKN-1) and its overall anticancer activity is slightly greater than that of oxaliplatin, whereas SPt-1 is less active than cisplatin. Moreover, the antitumor efficacy of SPt-2 on human colon carcinoma HCT-116 xenografts in nude mice is also greater than that of oxaliplatin, suggesting that SPt-2 deserves further evaluation as a prodrug for oxaliplatin.
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