Abstract

Chemical, pharmacological, and clinical research on anticancer coordination complexes has led to noteworthy anticancer drugs such as cisplatin, carboplatin and oxaliplatin. Although these compounds are effective chemotherapeutic agents in the treatment of different tumors, they are associated with high toxicity and numerous side effects. Several studies have shown that the range of platinum complexes with antitumor activity is not limited to structural analogs of cisplatin. Therefore, the development of convenient anticancer drugs that can be effectively used for the treatment of human tumors has become the main goal of most research groups in this field. In this sense, active platinum complexes without NH groups, transplatinum complexes, multinuclear complexes, cationic complexes, and several classes of palladium(II) complexes have emerged. Herein, the synthesis and characterization of two Pt(II) or Pd(II) complexes with PyTz (2-(2-pyridyl)iminotetrahydro-1,3-thiazine), a thiazine derivative ligand, with the formula [MCl2(PyTz)]·C2H6O (M = Pt(II) or Pd(II)) were reported. The potential anticancer ability of both complexes was evaluated in epithelial cervix carcinoma HeLa, human ovary adenocarcinoma SK-OV-3, human histiocytic lymphoma U-937, and human promyelocytic leukemia HL-60 cell lines. Interestingly, the Pt(II) complex showed great cytotoxic potential against all tumor cell lines tested, whereas the Pd(II) complex displayed slight antitumor actions.

Highlights

  • In the last few years, many promising advances have been achieved in the field of cancer treatment

  • + cations and four water molecules cells, each containing two chloride ions, two cells, each containing two chloride ions, two PyTzH cations and four water molecules of of crystallization. It be could be formulated as PyTz of the crystallization

  • RPMI-1640, McCoy0 s 5a, Dulbecco’s modified Eagle’s medium (DMEM), DMEM F-12, penicillin/streptomycin, foetal bovine serum (FBS), horse serum and L-glutamine were procured from ThermoFisher Scientific (Barcelona, Spain)

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Summary

Introduction

In the last few years, many promising advances have been achieved in the field of cancer treatment. The disease still widely affects humanity and remains to be the second leading cause of death after cardiovascular diseases [1]. A total of 8.8 million people died from cancer in 2015, and the number of new cases is expected to increase by approximately 70% over the twenty years [2]. Cisplatin (cis-diamminedichloroplatinum(II)), approved in 1978 for clinical use, is one of the most widely used complexes in anticancer therapy together with secondgeneration Pt complexes such as carboplatin (diammine(1,1-cyclobutanedicarboxylato(2-)O,O0 )platinum(II)), approved in 1993, or oxaliplatin (cis-[(1R,2R)-1,2-cyclohexanediammine-. N,N0 ][oxalato(2-)-O,O0 ]platinum(II)), approved in 2002 [3]. The square-planar Pt(II) complexes are activated by slow hydrolysis of the anionic ligands and the corresponding cationic aquo complexes formed bind to DNA creating stable intrachain cross-links that block replication and/or prevent transcription [4]

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