Novel quinoxaline derivatives as dual EGFR and COX-2 inhibitors: synthesis, molecular docking and biological evaluation as potential anticancer and anti-inflammatory agents.

ABSTRACT: Novel quinoxaline derivatives (2a-d, 3, 4a, 4b and 5-15) have been synthesized via the reaction of 4-methyl-3-oxo-3,4-dihydroquinoxaline-2-carbohydrazide (1) with different aldehydes, ketones, diketones, ketoesters, as well as hydrazine, phenyl isothiocyanate, carbon disulphide. The synthesized products have been screened for their in vitro anticancer and COX inhibitory activities. Most of the synthesized compounds exhibited good anticancer and COX-2 inhibitory activities. MTT assay revealed that compounds 11 and 13 were the most potent and exhibited very strong anticancer activity against the three cancer cell lines with IC₅₀ values ranging from 0.81 μM to 2.91 μM. Compounds 4a and 5 come next and displayed strong anticancer activity against the three cancer cell

SUBMITTER: Ahmed EA 

PROVIDER: S-EPMC9443684 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature