Abstract
A series of macrocyclic pyrido-pentapeptide candidates
⁻
were synthesized by using
,
-bis-[1-carboxy-2-(benzyl)]-2,6-(diaminocarbonyl)pyridine
,
as starting material. Structures of the newly synthesized compounds were established by IR, ¹H and
C-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,
showed encouraging inhibitory activity on MCF-7 and HepG-2 cell lines with IC
values 9.41 ± 1.25 and 7.53 ± 1.33 μM, respectively. Interestingly,
also demonstrated multitarget profile and excellent inhibitory activity towards VEGFR-2, CDK-2 and PDGFRβ kinases. Furthermore, molecular modeling studies of the compound
revealed its possible binding modes into the active sites of those kinases.