Thiazolation of phenylthiosemicarbazone to access new thiazoles: anticancer activity and molecular docking.

ABSTRACT: Aim: Novel thiazole hybrids were synthesized via thiazolation of 4-phenylthiosemicarbazone (4). Materials & methods: The anticancer activity against the NCI 60 cancer cell line panel. Results: Methyl 2-(2-((1-(naphthalen-2-yl)ethylidene)hydrazineylidene)-4-oxo-3-phenylthiazolidin-5-ylidene)acetate (6a) showed significant anticancer activity at 10 μM with a mean growth inhibition (GI) of 51.18%. It showed the highest cytotoxic activity against the ovarian cancer OVCAR-4 with an IC₅₀ of 1.569 ± 0.06 μM. Compound 6a inhibited PI3Kα with IC₅₀ = 0.225 ± 0.01 μM. Moreover, compound 6a revealed a decrease of Akt and mTOR phosphorylation in OVCAR-4 cells. In addition, antibacterial activity showed that compounds 11 and <

SUBMITTER: Elgammal WE 

PROVIDER: S-EPMC11247539 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature