Antiproliferative Activities of Cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] and its in vitro anti-VEGFR-2 Inhibition

Amr, A E; Elsayed, E A; Almehizia, A A; Wadaan, M A; Sabry, Nermien M; Baabbad, A


Research is continuing for synthesizing new molecules with potent pharmacological effects against cancer. In the current work we prepared a new tripeptide and investigated its in vitro as well as in vivo antiproliferative effects. Firstly, cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] was prepared and then tested against 17 different cancer cell lines. Results showed that the prepared compound showed increased cytotoxic effects (in terms of decreased IC50 value), which reached about 20.3, 28.1, 18.3 and 72.3% against RKOP27, K561, GOTO, HT1080 cell lines, respectively, in comparison to standard positive controls. Furthermore, cancer cell viability was probably affected through VEGFR-2 kinase inhibition.


Amino acid ester, Anticancer, Cyclic tripeptide, in vivo, Kinase inhibition, Macrocyclic

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