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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands.
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Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands.

机译:合成,对MCF-7细胞系的细胞毒活性以及具有2-取代的苯并咪唑配体的铂(II)配合物的诱变活性。

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摘要

Four Pt(II) complexes with 2-H/or-methyl/or-aminomethylbenzimidazole or 1,2-dimethylbenzimidazole ligands as "non-leaving groups" were synthesized and their antiproliferative properties were tested against the human MCF-7 breast cancer cell line. The mutagenic potentials of the complexes were tested in Salmonella typhimurium strains TA 98 and TA 100 in the absence of S9 rat liver fraction. In general, Pt(II) complexes tested which were found to be less active than cisplatin, exhibited moderate in vitro cytotoxic activity on MCF-7 cell line. Among the complexes tested, Pt(II) complex with 2-aminomethylbenzimidazole ligand was found to be highly mutagenic in S. typhimurium TA 98 and low mutagenic in S. typhimurium TA 100. Pt(II) complex with 1,2-dimethylbenzimidazole was mutagenic only in S. typhimurium TA 98. The other two complexes were found to be non-mutagen in both strains.
机译:合成了具有2-H /或甲基/或氨基甲基苯并咪唑或1,2-二甲基苯并咪唑配体作为“非离去基团”的四种Pt(II)配合物,并测试了它们对人MCF-7乳腺癌细胞系的抗增殖性能。在不存在S9大鼠肝组分的情况下,在鼠伤寒沙门氏菌TA 98和TA 100菌株中测试了复合物的诱变潜力。通常,发现测试的Pt(II)复合物的活性低于顺铂,对MCF-7细胞系表现出中等的体外细胞毒性活性。在测试的配合物中,发现具有2-氨基甲基苯并咪唑配体的Pt(II)配合物在鼠伤寒沙门氏菌TA 98中具有高致突变性,而在鼠伤寒沙门氏菌TA 100中具有低致突变性。具有1,2-二甲基苯并咪唑的Pt(II)配合物具有致突变性仅在鼠伤寒沙门氏菌TA 98中。在这两个菌株中发现其他两种复合物均为非诱变剂。

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