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新型炔基金(I)配合物的合成、细胞毒性及抗癌活性

Synthesis, cytotoxicity and anti-cancer activity of new alkynyl-gold(I) complexes.

作者信息

De Nisi Assunta, Bergamini Christian, Leonzio Marco, Sartor Giorgio, Fato Romana, Naldi Marina, Monari Magda, Calonghi Natalia, Bandini Marco

机构信息

Department of Chemistry "G. Ciamician", Alma Mater Studiorum - University of Bologna, Via Selmi 2, 40126 Bologna, Italy.

出版信息

Dalton Trans. 2016 Jan 28;45(4):1546-53. doi: 10.1039/c5dt02905h. Epub 2015 Dec 21.

Abstract

Alkynyl(triphenylphosphine)gold(i) complexes carrying variously substituted propargylic amines have been synthesized and fully characterized in solution and solid state. High levels of toxicity (i.e. micromolar range) were recognized for a series of cancer cell lines with particular emphasis on HT29, IGROV1, HL60 and I407. In particular the lead compound 3ab was identified as the most active compound in all cell lines (IC50: 1.7-7.9 μM).

摘要

已合成了带有各种取代炔丙胺的炔基(三苯基膦)金(I)配合物,并在溶液和固态下进行了全面表征。已确认一系列癌细胞系具有高毒性水平(即微摩尔范围),尤其着重于HT29、IGROV1、HL60和I407。特别是先导化合物3ab被确定为所有细胞系中活性最高的化合物(IC50:1.7 - 7.9 μM)。

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