3,5-Dimethyl-1-thiocarbamoylpyrazole and its Pd(II) complexes: Synthesis, spectral studies and antitumor activity

作者:Rocha F V; Barra C V; Netto A V G*; Mauro A E; Carlos I Z; Frem R C G; Ananias S R; Quilles M B; Stevanato A; da Rocha M C
来源:European Journal of Medicinal Chemistry, 2010, 45(5): 1698-1702.
DOI:10.1016/j.ejmech.2009.12.073

摘要

Complexes of the type [PdX(2)(tdmPz)] {X = Cl(-)(1) Br(-)(2); l(-)(3); SCN(-)(4); tdmPz = 1-thiocarbamoy1-3,5-dimethylpyrazole} have been synthesized and characterized. Compound 1 was formed from the reaction between [PdCl(2)(CH(3)CN)(2)] and 1-thiocarbamoy1-3,5-dimethylpyrazole. Complexes 2, 3 and 4 were obtained by metathesis of the chloro groups from 1 by bromide, iodide and thiocyanate ions, respectively. All the compounds and cisplatin have been tested in vitro by WIT assay for their cytotoxicity against three murine cancer cell lines: mammary adenocarcinoma (LM3 and LMM3) and lung adenocarcinoma (LP07) as well towards normal murine peritoneal exudate cells (PEC). Promising cytotoxic effect against LM3 has been found for 3 showing IC(50) equal to 24.5 mu M which is comparable to the value obtained for cisplatin (30.3 mu M).

  • 出版日期2010-5