新型吡啶基查尔酮的合成及其抗锥虫活性
Synthesis and antitrypanosomal activities of novel pyridylchalcones.
作者信息
Bhambra Avninder S, Ruparelia Ketan C, Tan Hoon L, Tasdemir Deniz, Burrell-Saward Hollie, Yardley Vanessa, Beresford Kenneth J M, Arroo Randolph R J
机构信息
School of Allied Health Sciences, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
Leicester School of Pharmacy, Faculty of Health and Life Sciences, De Montfort University, The Gateway, Leicester, LE1 9BH, UK.
出版信息
Eur J Med Chem. 2017 Mar 10;128:213-218. doi: 10.1016/j.ejmech.2017.01.027. Epub 2017 Jan 23.
A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).
合成了一系列新型吡啶基查耳酮，并针对布氏罗得西亚锥虫进行了筛选。其中八种显示出良好的活性，活性最强的8号化合物的IC值为0.29 μM。用人KB细胞进行的细胞毒性测试表明，该化合物具有良好的选择性，选择性指数为47。当该化合物库针对杜氏利什曼原虫进行测试时，未观察到明显活性。总之，吡啶基查耳酮是开发用于治疗人类非洲锥虫病（HAT）的新型化合物的有前景的先导物。
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