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甲氧基烷基取代茂金属的合成、表征及细胞毒性研究。

Synthesis, characterization and cytotoxicity studies of methoxy alkyl substituted metallocenes.

机构信息

Dipartimento di Chimica, Università di Salerno, Via Ponte don Melillo, 84084 Fisciano (SA), Italy.

出版信息

Eur J Med Chem. 2011 Jan;46(1):122-8. doi: 10.1016/j.ejmech.2010.10.021. Epub 2010 Oct 27.

Abstract

Five titanocene derivatives and one zirconium analogous, having cyclopentadienylethenylmethoxy ligand, were synthesized and fully characterized by NMR, FT-IR, and elemental analysis. Two of these complexes showed a good cytotoxic activity on human breast cancer (MCF-7) cell lines. Moreover, the half-titanocene disclosed also a good cytotoxic activity on human embryonic kidney (HEK-293). Additionally, a study on the rate of hydrolysis of these compounds showed that the leaving groups significantly affect the rate of hydrolysis of cyclopentadienyl groups too. The different activity of synthesized compounds was tentatively related to the rate of hydrolysis.

摘要

合成了 5 种二茂钛衍生物和 1 种锆类似物,它们都具有环戊二烯基乙烯基甲氧基配体,并通过 NMR、FT-IR 和元素分析进行了充分的表征。其中两种配合物对人乳腺癌(MCF-7)细胞系表现出良好的细胞毒性活性。此外,半钛茂对人胚肾(HEK-293)也表现出良好的细胞毒性活性。此外,对这些化合物水解速率的研究表明,离去基团也显著影响环戊二烯基的水解速率。所合成化合物的不同活性与水解速率有关。

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