Issue 5, 2022

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

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 (Ep) 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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
08 Jan 2022
Accepted
07 Mar 2022
First published
18 Mar 2022

RSC Med. Chem., 2022,13, 594-598

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

A. Gao, Y. Wu, J. Yu, H. Gong, J. Jiang, C. Yang, W. Liu and C. Qing, RSC Med. Chem., 2022, 13, 594 DOI: 10.1039/D2MD00004K

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