Investigation of Growth Inhibitory Effects of cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornthenyl acid hydrazide] on Various Cancer Cells as well as in vitro VEGFR-2 Kinase Inhibition

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

Abstract

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.



Keyword(s)

Azide method, Cell lines, In vitro, In vivo, Kinase activity, Macrocyclic tripeptidopyridine


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