Anti-VEGFR-2 Kinase Effects of Cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)- L-lysine] and its Anticancer Activities Against Different Cancer Cell Lines

Amr, A E; Elsayed, E A; Al-Omar, M A; El-Enshasy, H A

Abstract

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.


Keyword(s)

Cyclic tripeptides; Pyridine derivatives; Anticancer; Animal model; Inhibition of VEGFR-2 tyrosine kinase

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