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Cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysinyl acid hydrazide]: Assessment of its Role in Cancer and Kinase Activity Inhibition
Journal of Scientific & Industrial Research ( IF 0.7 ) Pub Date : 2020-05-15
A E Amr, E A Elsayed, M A Al-Omar, A A Almehizia, Randa E. Abdel-Mageid

Current research aimed at evaluating the in vitro as well as in vivo anticancer activities of a newly synthesized peptide hydrazide; i.e. 4,14-diisopropyl-2,5,13,16-tetraoxo-3,6,12,15-tetraaza-1(3,5)-pyridinacyclohexadecaphane-7-carbohydrazide. The hydrazide was synthesized from methyl 4,14-diisopropyl-2,5,13,16-tetraoxo-3,6,12,15-tetraaza-1(3,5)-pyridinacyclohexadecaphane-7-carboxylate 2 by acting of hydrazine hydrate. It showed significant anticancer effects against different tested cell lines, where cervical, breast, liver, colon, prostate, brain, fibrosarcoma, leukemia and melanoma cell lines were the most affected cell types. The prepared derivative also inhibited VEGF-2 kinase enzyme significantly and exhibited an in vivo tumorigenic effects in mice model.

中文翻译:

环(Nα-二烟酰基)-双-[(L-缬氨酰基)-L-赖氨酰酰肼]:评估其在癌症和激酶活性抑制中的作用

当前的研究旨在评估新合成的肽酰肼的体外以及体内抗癌活性;即4,14-二异丙基-2,5,13,​​16-四氧代-3,6,12,15-四氮杂-1(3,5)-吡啶基环六癸烷-7-碳酰肼。通过水合肼的作用由4,4-二异丙基-2,5,13,​​16-四氧代-3,6,12,15-四氮杂-1(3,5)-吡啶基环六癸烷-7-羧酸酯2合成酰肼。它显示出对不同测试细胞系的显着抗癌作用,其中宫颈,乳腺癌,肝,结肠,前列腺,脑,纤维肉瘤,白血病和黑色素瘤细胞系是受影响最大的细胞类型。制备的衍生物还显着抑制VEGF-2激酶,并在体内表现出 在小鼠模型中具有致瘤作用。
更新日期:2020-05-15
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