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Antitumour Studies of Aluminium Complexes of Synthetic Curcuminoids

机译:合成姜黄素铝配合物的抗肿瘤研究

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Four curcuminoid analogues, namely 1 ,7-dianthryl-l ,6-heptadiene-3,5-dione,Ia;_1,7-bis(2- hydroxynapthyl}-1 ,6- heptadiene-3 ,5-dione,1b;1,7-bis(4-hydroxy-3-methoxyphenyl)- | ,6-heptadiene-3,5-dione, le; 1,7bis (4-methoxyphenyl)- | ,6-heptadiene-3,5-dione,ld and their aluminium (III) complexes of ML, stoichiometry were synthesized and characterized by UV, IR, 'H NMR and mass spectral data. The compounds were investigated for their possible cytotoxic and antitumour activities. It was found that aluminium chelates are remarkably active compared to free curcuminoid analogues. All the compounds were found to be cytotoxic towards Ehrlich ascites carcinoma cells and cultured L929 cells. In the case of culture studies, concentrations needed for 50% cell death were around 4ug/ml for aluminium complexes and |0yg/ml for curcuminoid analogues. Aluminium complex of 1b with hydroxyl group in the naphthyl ring was found to be most active towards L929cells (1 g/ml produced 62.5+1.9% cell death). Compound 1a which is the unsubstituted analogue is found to be the least active compound towards increase in life span of tumour-bearing mice (percentage increase in life span is 29.5). Aluminium chelates of all curcuminoid.
机译:四种姜黄素类似物,即1,7-二蒽-1,6-庚二烯-3,5-二酮,Ia; _1,7-双(2-羟基萘基)-1,6-庚二烯-3,5-二酮,1b; 1,7-双(4-羟基-3-甲氧基苯基)-|,6-庚二烯-3,5-二酮,le; 1,7双(4-甲氧基苯基)-|,6-庚二烯-3,5-二酮,合成了1d及其分子结构ML,化学计量的铝(III)配合物,并通过UV,IR,1H NMR和质谱数据进行了表征,研究了这些化合物可能的细胞毒性和抗肿瘤活性,发现铝螯合物具有显着的活性。与游离姜黄素类似物相比,所有化合物均对艾氏腹水癌细胞和培养的L929细胞具有细胞毒性,在培养研究中,铝复合物50%细胞死亡所需的浓度约为4ug / ml,| 0yg /对于姜黄素类似物,每毫升1毫升的铝配合物在萘环上具有羟基,被发现对L929细胞最具活性(1克/毫升产生62.5 + 1.9%的细胞死亡)。发现未取代的类似物磅1a是对荷瘤小鼠寿命延长的最小活性化合物(寿命延长百分比为29.5)。所有姜黄素的铝螯合物。

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