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. 2022 Mar 18;13(5):594-598.
doi: 10.1039/d2md00004k. eCollection 2022 May 25.

Synthesis and anticancer activity of two highly water-soluble and ionic Pt(iv) complexes as prodrugs for Pt(ii) anticancer drugs

Anli Gao  1 , Yaxi Wu  2   3 , Juan Yu  1 , Hongyu Gong  2 , Jing Jiang  1 , Caihong Yang  2 , Weiping Liu  1 , Chen Qing  2
Affiliations

Synthesis and anticancer activity of two highly water-soluble and ionic Pt(iv) complexes as prodrugs for Pt(ii) anticancer drugs

Anli Gao et al. RSC Med Chem. .

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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Conflict of interest statement

The authors declare that they have no conflict of interest.

Figures

Fig. 1
Fig. 1. Chemical structures of platinum(iv) agents that have undergone clinical trials.
Fig. 2
Fig. 2. The chemical structures of SPt-1 and SPt-2.
Fig. 3
Fig. 3. Cyclic voltammograms for the blank solution (Na2SO4), SPt-1 and SPt-2 measured in aqueous solution.
See this image and copyright information in PMC

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