During the current work, we synthesized a new peptide derivative; 4,13-diisopropyl-2,5,12,15-tetraoxo-3,6,11,14-tetraaza-1(3,5)-pyridinacyclopentadecaphane-7-carbohydrazide. The prepared hydrazide was investigated for its in vivo as well as in vitro anticancer effects. Results revealed that this derivative has a great potential against 6 cancerous cell lines. Furthermore, the highest effect was obtained against HT1080 and HeLa cells, where the compound showed 7.4- and 15.1-folds increased activity against them, respectively. Additionally, the compound seems to exert its potential anticancer effect by affecting the kinase enzyme VEGFR-2. Finally, the compound showed promising results when tested in in vivo against prostate cancer developed animal models.

中文翻译：

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环（Nα-吡啶基）-双-[[（L-缬氨酰基）-L-烯基酸酰肼]对多种癌细胞的生长抑制作用以及体外VEGFR-2激酶抑制作用的研究

在当前的工作中，我们合成了一种新的肽衍生物。4,13-二异丙基-2,5,12,15-四氧代-3,6,11,14-四氮杂-1（3,5）-吡啶基环戊癸烷-7-碳酰肼。研究了所制备的酰肼的体内和体外抗癌作用。结果表明，该衍生物具有对抗6种癌细胞的巨大潜力。此外，针对HT1080和HeLa细胞获得了最高的效果，其中该化合物对HT1080和HeLa细胞的活性分别提高了7.4倍和15.1倍。此外，该化合物似乎通过影响激酶VEGFR-2发挥其潜在的抗癌作用。最后，当在体内针对前列腺癌开发的动物模型进行测试时，该化合物显示出令人鼓舞的结果。