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含4-羟基吖啶的环钯配合物的合成及抗癌活性

Synthesis and anticancer activity of cyclopalladated complexes containing 4-hydroxy-acridine.

作者信息

Pucci Daniela, Albertini Veronica, Bloise Rossana, Bellusci Anna, Cataldi Antonella, Catapano Carlo V, Ghedini Mauro, Crispini Alessandra

机构信息

Centro di Eccellenza CEMIF.CAL-LASCAMM, CR-INSTM Unità della Calabria, Dipartimento di Chimica, Università della Calabria, Italy.

出版信息

J Inorg Biochem. 2006 Sep;100(9):1575-8. doi: 10.1016/j.jinorgbio.2006.04.009. Epub 2006 May 5.

Abstract

The synthesis and the characterization (elemental analysis, (1)H NMR and X-ray) of the first cyclopalladated complexes containing 4-hydroxyacridinate as complementary ligand are described. 4-Hydroxyacridine acts as a bidentate [N,O] chelating ligand, giving rise to square planar Pd(II) complexes in the coordination of a cyclopalladated fragment of phenylpyridine or phenylpyrimidine, characterized by the presence of two almost coplanar metalated rings. The biological activity studies conducted on these new Pd(II) complexes proved that the phenylpyridine Pd(II) derivative is more efficient than cis-platinum. The intrinsically substitutional inertness of the cyclopalladated ring and the presence of the [N,O] chelated acridine ligand make these systems of particular interest in their promising biological activity.

摘要

本文描述了首例含有4-羟基吖啶作为辅助配体的环钯配合物的合成与表征(元素分析、¹H NMR和X射线)。4-羟基吖啶作为双齿[N,O]螯合配体,在苯基吡啶或苯基嘧啶的环钯片段配位中形成平面正方形的Pd(II)配合物,其特征是存在两个几乎共面的金属化环。对这些新型Pd(II)配合物进行的生物活性研究表明,苯基吡啶Pd(II)衍生物比顺铂更有效。环钯环的固有取代惰性以及[N,O]螯合吖啶配体的存在,使得这些体系因其有前景的生物活性而特别引人关注。

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