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含2-取代苯并咪唑配体的铂(II)配合物的合成、对MCF-7细胞系的细胞毒性活性及诱变活性

Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands.

作者信息

Gümüş Fatma, Algül Oztekin, Eren Gökçen, Eroğlu Hatice, Diril Nuran, Gür Sibel, Ozkul Aykut

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Gazi, 06330 Etiler, Ankara, Turkey.

出版信息

Eur J Med Chem. 2003 May;38(5):473-80. doi: 10.1016/s0223-5234(03)00058-8.

Abstract

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.

摘要

合成了四种以2 - H/邻甲基/邻氨甲基苯并咪唑或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特性。在不存在S9大鼠肝匀浆的情况下,在鼠伤寒沙门氏菌TA 98和TA 100菌株中测试了这些配合物的诱变潜力。一般来说,所测试的Pt(II)配合物被发现活性低于顺铂,对MCF - 7细胞系表现出中等程度的体外细胞毒性活性。在所测试的配合物中,带有2 - 氨甲基苯并咪唑配体的Pt(II)配合物在鼠伤寒沙门氏菌TA 98中具有高度诱变性,在鼠伤寒沙门氏菌TA 100中具有低诱变性。带有1,2 - 二甲基苯并咪唑的Pt(II)配合物仅在鼠伤寒沙门氏菌TA 98中具有诱变性。发现另外两种配合物在两种菌株中均无诱变性。

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