Cancer is a major risk disease affecting human survival. The pharmaceutical companies are continuing searching for new drug candidates with promising anticancer activities, and reduced side effects. The current work aimed at synthesized a new tripeptide with potential pharmacological properties. L-Valine methyl ester was used to prepare cyclo (N^α-dinicotinoyl)-bis-[(L-valinyl)-L-lysine methyl ester. The new compound revealed promising in vitro cytotoxic activities against different neuroblastoma, cervical carcinoma, fibrosarcoma as well as hepatocellular carcinomas. Furthermore, we also found that the obtained IC₅₀ of the compound decreased by about 50% during its in vivo anti-prostate cancer evaluation. Furthermore, the mechanism of action studies proposes that the new prepared derivative affects cancer cells trough the inhibition of VEGFR-2 kinase enzyme.

中文翻译：

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新合成的环（Nα-二烟酰基）-双-[（L-缬氨酰基）-L-赖氨酸甲基酯]的体外和体内细胞毒性活性和激酶抑制作用的评估

癌症是影响人类生存的主要危险疾病。制药公司正在继续寻找具有前途的抗癌活性并减少副作用的新药。当前的工作旨在合成具有潜在药理特性的新三肽。L-缬氨酸甲酯来制备环（Ñ ^α -dinicotinoyl） -双- [（L缬氨酰）-L-赖氨酸甲酯。新化合物显示出对不同的神经母细胞瘤，宫颈癌，纤维肉瘤以及肝细胞癌有希望的体外细胞毒性活性。此外，我们还发现，化合物的体内IC ₅₀降低了约50％抗前列腺癌评估。此外，作用机理研究表明，新制备的衍生物通过抑制VEGFR-2激酶来影响癌细胞。