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对 p-甲苯乙酸的自组装有机锡(IV)酯的结构阐明及其对细菌、真菌、卤虫和土豆肿瘤细胞的抑制作用。

Structure elucidation and inhibitory effects of self-assembled organotin(IV) esters of p-tolyl acetic acid on bacterial, fungal, brine shrimp, and potato tumor cells.

机构信息

Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.

出版信息

Drug Chem Toxicol. 2010 Apr;33(2):183-92. doi: 10.3109/01480540903203992.

Abstract

Biologically active new organotin(IV) acetates (1-6) of p-tolyl acetic acid have been synthesized and characterized by multinuclear nuclear magnetic resonance ((1)H, (13)C) and mass spectrometry. The X-ray crystallographic data of compounds (3 and 4) were also collected. These studies show that in diorganotin(IV) compounds (compounds 1, 2, 3, and 6), tin exists in skew trapezoidal geometry with four strong and two weaker bonds, whereas triorganotin(IV) carboxylates (compounds 4 and 5) have four and five coordinated geometries in solution and solid form, respectively. These compounds were screened for a range of biological activities. Antibacterial activities were determined against six pathogenic bacterial strains, three Gram-positive and three Gram-negative; the activities were measured in terms of inhibition zones (mm). Antifungal activities were determined against six pathogenic fungal strains, cytotoxicity by the brine shrimp lethality assay, and antitumor activities by the crown gall tumor inhibition (potato disc) assay.

摘要

已经合成了具有生物活性的新的有机锡(IV)对甲苯乙酸盐(1-6),并通过多核核磁共振(1H、13C)和质谱进行了表征。还收集了化合物(3 和 4)的 X 射线晶体学数据。这些研究表明,在二有机锡(IV)化合物(化合物 1、2、3 和 6)中,锡以斜梯形几何形状存在,具有四个强键和两个较弱键,而三有机锡(IV)羧酸盐(化合物 4 和 5)在溶液中和固体形式中分别具有四配位和五配位几何形状。这些化合物进行了一系列生物活性筛选。针对六种病原菌进行了抗菌活性测定,其中三种为革兰氏阳性菌,三种为革兰氏阴性菌;抗菌活性通过抑菌圈(mm)来衡量。针对六种病原菌进行了抗真菌活性测定,采用卤虫致死试验测定细胞毒性,采用冠瘿瘤抑制(马铃薯圆盘)试验测定抗肿瘤活性。

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