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2-氧代-1,2-二氢喹啉-3-甲醛缩氨硫脲末端氮原子取代对其钯(II)配合物配位行为、结构和生物性能的影响。

Role of substitution at terminal nitrogen of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde thiosemicarbazones on the coordination behavior and structure and biological properties of their palladium(II) complexes.

机构信息

Department of Chemistry, Bharathiar University, Coimbatore 641046 India.

出版信息

Inorg Chem. 2013 Feb 4;52(3):1504-14. doi: 10.1021/ic302258k. Epub 2013 Jan 16.

Abstract

A series of four new palladium(II) complexes of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde thiosemicarbazones with triphenylphosphine as coligand have been synthesized and characterized by the aid of various spectral techniques. The single-crystal X-ray diffraction studies revealed that the unsubstituted thiosemicarbazone ligand acted as monobasic tridentate (ONS(-)) in the cationic [Pd(H-Qtsc-H)(PPh(3))]Cl complex, whereas the monosubstituted thiosemicarbazone ligands acted as monobasic bidentate (NS(-)) in their respective complexes, [PdCl(H-Qtsc-R)(PPh(3))] (R = Me (2), Et (3), Ph (4)). To ascertain the potentials of the above Pd(II) complexes toward biomolecular interactions, additional experiments involving interaction with calf thymus DNA and bovine serum albumin were carried out. Moreover, all the palladium(II) complexes have been screened for their radical scavenging activity toward DPPH, O(2)(-), OH, and NO radicals. The efficiency of the complexes in arresting the growth of human cervical cancer cells (HeLa), human laryngeal epithelial carcinoma cells (HEp-2), human liver carcinoma cells (Hep G2), and human skin cancer cells (A431) has also been studied along with the cell viability test against the noncancerous NIH 3T3 mouse embryonic fibroblasts cell lines under in vitro conditions. All the in vitro pharmacological evaluation results clearly revealed the relationship between the structure and the activity of the new Pd(II) complexes.

摘要

一系列四种新的钯(II)配合物的 2-氧代-1,2-二氢喹啉-3-甲酰腙硫代半卡巴腙与三苯基膦作为配位体已经被合成和各种光谱技术的特点。单晶 X 射线衍射研究表明,未取代的硫代半卡巴腙配体在阳离子[Pd(H-Qtsc-H)(PPh3)]Cl 配合物中作为单齿三配位(ONS(-)),而单取代的硫代半卡巴腙配体在各自的配合物中作为单齿双配位(NS(-)),[PdCl(H-Qtsc-R)(PPh3)](R=Me(2),Et(3),Ph(4))。为了确定上述 Pd(II)配合物对生物分子相互作用的潜力,进行了额外的与小牛胸腺 DNA 和牛血清白蛋白相互作用的实验。此外,所有钯(II)配合物都被筛选出对 DPPH、O2(-)、OH 和 NO 自由基的清除活性。还研究了这些配合物在体外条件下对人宫颈癌(HeLa)细胞、人喉上皮癌细胞(HEp-2)、人肝癌细胞(Hep G2)和人皮肤癌细胞(A431)生长的抑制作用,以及对非癌细胞 NIH 3T3 小鼠胚胎成纤维细胞系的细胞活力测试。所有的体外药理评价结果清楚地揭示了新的 Pd(II)配合物的结构和活性之间的关系。

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