3,5-二甲基-1-硫代羰基吡唑及其 Pd(II) 配合物的合成、光谱研究及抗肿瘤活性。
3,5-Dimethyl-1-thiocarbamoylpyrazole and its Pd(II) complexes: synthesis, spectral studies and antitumor activity.
机构信息
Departamento de Química Geral e Inorgânica, Instituto de Química de Araraquara, UNESP-University Estadual Paulista, P.O. Box 355, Araraquara, São Paulo 14801-970, Brazil.
出版信息
Eur J Med Chem. 2010 May;45(5):1698-702. doi: 10.1016/j.ejmech.2009.12.073. Epub 2010 Jan 14.
Complexes of the type [PdX2(tdmPz)] {X=Cl-(1), Br-(2); I-(3); SCN-(4); tdmPz=1-thiocarbamoyl-3,5-dimethylpyrazole} have been synthesized and characterized. Compound 1 was formed from the reaction between [PdCl2(CH3CN)2] and 1-thiocarbamoyl-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 MTT 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 IC50 equal to 24.5 microM which is comparable to the value obtained for cisplatin (30.3 microM).
已经合成并表征了[PdX2(tdmPz)]类型的配合物，其中 X=Cl-(1)，Br-(2)，I-(3)，SCN-(4)，tdmPz=1-硫代羰酰基-3,5-二甲基吡唑。化合物 1 是由[PdCl2(CH3CN)2]与 1-硫代羰酰基-3,5-二甲基吡唑反应生成的。配合物 2、3 和 4 是通过 1 中氯原子的转移反应由溴化物、碘化物和硫氰酸根离子分别得到的。所有化合物和顺铂都通过 MTT 测定法在体外对三种鼠癌细胞系（乳腺腺癌（LM3 和 LMM3）和肺腺癌（LP07））以及对正常鼠腹腔渗出细胞（PEC）的细胞毒性进行了测试。发现 3 对 LM3 具有有前途的细胞毒性作用，其 IC50 为 24.5 microM，与顺铂（30.3 microM）的值相当。
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