Journal
MOLECULES
Volume 23, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/molecules23102416
Keywords
macrocyclic pentapeptides; in vitro anticancer activity; multitarget; molecular modeling studies
Funding
- Deanship of Scientific Research, King Saud University [RGP-1435-047]
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A series of macrocyclic pyrido-pentapeptide candidates 2-6 were synthesized by using N,N-bis-[1-carboxy-2-(benzyl)]-2,6-(diaminocarbonyl)pyridine 1a,b as starting material. Structures of the newly synthesized compounds were established by IR, H-1 and C-13-NMR, and MS spectral data and elemental analysis. The in-vitro cytotoxicity activity was investigated for all compounds against MCF-7 and HepG-2 cell lines and the majority of the compounds showed potent anticancer activity against the tested cell lines in comparison with the reference drugs. Out of the macrocyclic pyrido-pentapeptide based compounds, 5c showed encouraging inhibitory activity on MCF-7 and HepG-2 cell lines with IC50 values 9.41 +/- 1.25 and 7.53 +/- 1.33 mu M, respectively. Interestingly, 5c also demonstrated multitarget profile and excellent inhibitory activity towards VEGFR-2, CDK-2 and PDGFR beta kinases. Furthermore, molecular modeling studies of the compound 5c revealed its possible binding modes into the active sites of those kinases.
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