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Anti-VEGFR-2 Kinase Effects of Cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)- L-lysine] and its Anticancer Activities Against Different Cancer Cell Lines
Journal of Scientific & Industrial Research ( IF 0.6 ) Pub Date : 2020-07-09
A E Amr, E A Elsayed, M A Al-Omar, H A El-Enshasy

The current work aimed at preparing a cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysine] from previously established synthetic routs. The derivative was investigated for its potential anticancer activities as well as its possible mechanism of action. The prepared compound showed variable anticancer activities against all tested cell lines. Furthermore, it showed very promising activities in terms of obtained IC50 values compared to known used drugs. The mechanism of action studies showed that the prepared tripeptide may act on cancerous cells through its inhibitory action on tyrosine kinase pathway. Animal model experiments proved the potential of the synthesized tripeptide as an anticancer agent against PC3 cancer cells.

中文翻译:

环(Nα-二烟酰基)-双-[((L-缬氨酰基)-L-赖氨酸]的抗VEGFR-2激酶作用及其对不同癌细胞系的抗癌活性

旨在制备一个环(在当前工作Ñ α -dinicotinoyl) -双-从先前建立的合成击溃[(L缬氨酰)-L-赖氨酸]。研究了该衍生物的潜在抗癌活性及其可能的作用机理。制备的化合物对所有测试的细胞系显示出可变的抗癌活性。此外,与已知的二手药物相比,它在获得的IC50值方面显示出非常有希望的活性。作用机理研究表明,所制备的三肽可能通过对酪氨酸激酶途径的抑制作用而作用于癌细胞。动物模型实验证明了合成的三肽作为抗PC3癌细胞的抗癌剂的潜力。
更新日期:2020-07-28
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