Kekecmuhammed, HuseyinTapera, MichaelAydogdu, EkremSaripinar, EminKaratas, Elanur AydinUc, Eda MehtapAkyuz, Mesut2024-10-262024-10-2620231612-18721612-1880https://doi.org/10.1002/cbdv.202200886https://hdl.handle.net/20.500.12418/30104In an attempt to identify potential active anticancer agents with low cytotoxic properties and CA inhibitors, a new series of hybrid compounds incorporating imidazole ring and hydrazone moiety as part of their structure were synthesized by aza-Michael addition reaction followed by intramolecular cyclization. The structure of synthesized compounds was elucidated using various spectral techniques. Synthesized compounds were evaluated for their in vitro anticancer (prostate cell lines; PC3) and CA inhibitory (hCA I and hCA II) activity. Among them, some compound displayed remarkable anticancer activity and CA inhibitory activity with K-i values in range of 17.53 +/- 7.19-150.50 +/- 68.87 nM against cytosolic hCA I isoform associated with epilepsy, and 28.82 +/- 14.26-153.27 +/- 55.80 nM against dominant cytosolic hCA II isoforms associated with glaucoma. Furthermore, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness qualities. The proteins used for the calculations are prostate cancer protein (PDB ID: 3RUK and 6XXP). ADME/T analysis was carried out to examine the drug properties of the studied molecules.en10.1002/cbdv.202200886info:eu-repo/semantics/closedAccessanticancer agentcarbonic anhydrase inhibitorshydrazoneimidazolesynthesisArticle206371321912-s2.0-85159895426Q2WOS:000991681000001Q3