一些新型N'-(2-氧代吲哚啉-3-亚基)-2-丙基戊烷酰肼腙衍生物的合成、表征及抗癌活性
Synthesis, Characterization, and Anti-Cancer Activity of Some New N'-(2-Oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazones Derivatives.
作者信息
El-Faham Ayman, Farooq Muhammad, Khattab Sherine N, Abutaha Nael, Wadaan Mohammad A, Ghabbour Hazem A, Fun Hoong-Kun
机构信息
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria 21321, Egypt.
出版信息
Molecules. 2015 Aug 13;20(8):14638-55. doi: 10.3390/molecules200814638.
Eight novel N'-(2-oxoindolin-3-ylidene)-2-propylpentane hydrazide-hydrazone derivatives 4a-h were synthesized and fully characterized by IR, NMR ((1)H-NMR and (13)C-NMR), elemental analysis, and X-ray crystallography. The cyto-toxicity and in vitro anti-cancer evaluation of the prepared compounds have been assessed against two different human tumour cell lines including human liver (HepG2) and leukaemia (Jurkat), as well as in normal cell lines derived from human embryonic kidney (HEK293) using MTT assay. The compounds 3e, 3f, 4a, 4c, and 4e revealed promising anti-cancer activities in tested human tumour cells lines (IC50 values between 3 and 7 μM) as compared to the known anti-cancer drug 5-Fluorouracil (IC50 32-50 μM). Among the tested compounds, 4a showed specificity against leukaemia (Jurkat) cells, with an IC50 value of 3.14 μM, but this compound was inactive in liver cancer and normal cell lines.
合成了八种新型的N'-(2-氧代吲哚啉-3-亚基)-2-丙基戊烷酰肼腙衍生物4a-h，并通过红外光谱、核磁共振（(1)H-NMR和(13)C-NMR）、元素分析和X射线晶体学对其进行了全面表征。使用MTT法对所制备化合物针对两种不同的人类肿瘤细胞系（包括人肝癌细胞系（HepG2）和白血病细胞系（Jurkat））以及源自人胚胎肾的正常细胞系（HEK293）进行了细胞毒性和体外抗癌评估。与已知抗癌药物5-氟尿嘧啶（IC50为32-50 μM）相比，化合物3e、3f、4a、4c和4e在测试的人类肿瘤细胞系中显示出有前景的抗癌活性（IC50值在3至7 μM之间）。在所测试的化合物中，4a对白血病（Jurkat）细胞具有特异性，IC50值为3.14 μM，但该化合物在肝癌细胞系和正常细胞系中无活性。
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