Coumarin-amino acid hybrids as promising anticancer agents: design, synthesis, docking studies and CK2 inhibition.

ABSTRACT: A series of mono-peptide, di-peptide and tri-peptide derivatives linked to a coumarin scaffold (5a-c, 7a-c, and 9a-c) were synthesized via the azide-coupling method from corresponding hydrazides 4, 6, and 8. These compounds were tested for anticancer activity against HepG-2, PC-3, and Hct-116 cell lines. Compounds, 7c, and 5b showed significant cytotoxicity, outperforming doxorubicin, with IC₅₀ values of 34.07, 16.06, and 16.02 μM for 7c and 42.16, 59.74, and 35.05 μM for 5b. Compound 7b also displayed promising results with IC₅₀ values of 72.13, 70.82, and 61.01 μM. Moreover, the key structural features of amino acids indicated that mono-peptide and di-peptide derivatives play a key role in increasing their anticancer activities compared with tri-peptides. In

SUBMITTER: El-Etrawy AS 

PROVIDER: S-EPMC11302324 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature