Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B.

ABSTRACT: A library of monosubstituted chalcones (1-17) bearing electron-donating and electron-withdrawing groups on both aromatic rings were selected. The cell viability on human tumor cell lines was evaluated first. The compounds unable to induce detectable cytotoxicity (1, 13, and 14) were tested using the monoamine oxidase (MAO) activity assay. Interestingly, they inhibit MAO-B, acting as competitive inhibitors, with 13 and 14 showing the best profiles. In particular, 13 exhibited a potency higher than that of safinamide, taken as a reference. Docking studies and crystallographic analysis showed that in human MAO-B 13 binds with the halogen-substituted aromatic ring in the entrance cavity, similar to safinamide, whereas 14 is

SUBMITTER: Iacovino LG 

PROVIDER: S-EPMC8274062 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature