Ullah, Sultan published the artcileThe tyrosinase-inhibitory effects of 2-phenyl-1,4-naphthoquinone analogs: importance of the (E)-β-phenyl-α,β-unsaturated carbonyl scaffold of an endomethylene type, Related Products of isoquinoline, the main research area is phenylnaphthoquinone endomethylene synthesis tyrosinase skin whitening melanogenesis.
In order to investigate the effect of the (E)-β-phenyl-α,β-unsaturated carbonyl scaffold of an endomethylene type on tyrosinase inhibition, 2-phenyl-1,4-naphthoquinone derivatives were synthesized by Michael addition of substituted benzenes to 1,4-naphthoquinone and subsequently an auto-oxidation Most of the derivatives potently inhibited mushroom tyrosinase and four derivatives, including 1c (IC50 = 22.00 ± 1.63 μM), more potently inhibited mushroom tyrosinase than kojic acid (IC50 = 37.86 ± 2.21 μM). Cell-based assays using B16F10 cells (a melanoma cell line) showed 1c dose-dependently suppressed melanin production and more potently inhibited tyrosinase activity than kojic acid. Docking simulation results between 1c and tyrosinase and a kinetic study suggest that 1c is a competitive inhibitor that binds to the active site of tyrosinase. These results support that anti-melanogenic effect of naphthoquinone derivatives results from their tyrosinase inhibiting activity and the (E)-β-phenyl-α,β-unsaturated carbonyl scaffold of an endomethylene type can confer tyrosinase-inhibitory activity.
Medicinal Chemistry Research published new progress about Enzyme inhibitors. 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, Related Products of isoquinoline.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem