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A Novel Approach for Bisphosphonates: Ionic Liquids and Organic Salts from Zoledronic Acid.
ChemMedChem ( IF 3.6 ) Pub Date : 2019-10-11 , DOI: 10.1002/cmdc.201900397
Sónia Teixeira 1, 2 , Miguel M Santos 2 , Ricardo Ferraz 3, 4 , Cristina Prudêncio 3, 5 , Maria H Fernandes 1, 6 , João Costa-Rodrigues 1, 5, 7 , Luís C Branco 2
Affiliation  

Novel ionic liquids and organic salts based on mono- or dianionic zoledronate and protonated superbases, choline and n-alkylmethylimidazolium cations, were prepared and characterized by spectroscopic and thermal analyses. Most of the prepared salts display amorphous structures and very high solubility in water and saline solutions, especially the dianionic salts. Among the zoledronate-based ionic compounds, those containing choline [Ch] and methoxyethylmethylimidazolium [C3 OMIM] cations appear to have significant cytotoxicity against human osteosarcoma cells (MG63) and low toxicity toward healthy skin fibroblast cells. Because osteosarcoma is a bone pathology characterized by an increase in bone turnover rate, the results presented herein may be a promising starting point for the development of new ionic pharmaceutical drugs against osteosarcoma.

中文翻译:

双膦酸盐的新方法:唑来膦酸的离子液体和有机盐。

制备了基于单或双阴离子唑来膦酸盐和质子化的超碱,胆碱和正烷基甲基咪唑鎓阳离子的新型离子液体和有机盐,并通过光谱和热分析对其进行了表征。多数制备的盐显示出无定形结构,并且在水和盐溶液中的溶解度非常高,尤其是二价阴离子盐。在基于唑来膦酸盐的离子化合物中,那些含有胆碱[Ch]和甲氧基乙基甲基咪唑鎓[C3 OMIM]阳离子的化合物似乎对人骨肉瘤细胞(MG63)具有明显的细胞毒性,对健康的皮肤成纤维细胞的毒性低。因为骨肉瘤是一种以骨转换率增加为特征的骨病理学,所以本文介绍的结果可能是开发抗骨肉瘤的新型离子药物的有前途的起点。
更新日期:2019-10-12
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