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dc.contributor.authorYasir Naziren_US
dc.contributor.authorHummera Rafiqueen_US
dc.contributor.authorNaghmana Kausaren_US
dc.contributor.authorQamar Abbasen_US
dc.contributor.authorZaman Ashrafen_US
dc.contributor.authorPornchai Rachtanapunen_US
dc.contributor.authorKittisak Jantanasakulwongen_US
dc.contributor.authorWarintorn Ruksiriwanichen_US
dc.description.abstractTargeting tyrosinase for melanogenesis disorders is an established strategy. Hydroxyl-substituted benzoic and cinnamic acid scaffolds were incorporated into new chemotypes that displayed in vitro inhibitory effects against mushroom and human tyrosinase for the purpose of identifying anti-melanogenic ingredients. The most active compound 2-((4-methoxyphenethyl)amino)-2-oxoethyl (E)-3-(2,4-dihydroxyphenyl) acrylate (Ph9), inhibited mushroom tyrosinase with an IC50 of 0.059 nM, while 2-((4-methoxyphenethyl)amino)-2-oxoethyl cinnamate (Ph6) had an IC50 of 2.1 nM compared to the positive control, kojic acid IC50 16700 nM. Results of human tyrosinase inhibitory activity in A375 human melanoma cells showed that compound (Ph9) and Ph6 exhibited 94.6% and 92.2% inhibitory activity respectively while the positive control kojic acid showed 72.9% inhibition. Enzyme kinetics reflected a mixed type of inhibition for inhibitor Ph9 (Ki 0.093 nM) and non-competitive inhibition for Ph6 (Ki 2.3 nM) revealed from Lineweaver–Burk plots. In silico docking studies with mushroom tyrosinase (PDB ID:2Y9X) predicted possible binding modes in the catalytic site for these active compounds. Ph9 displayed no PAINS (pan-assay interference compounds) alerts. Our results showed that compound Ph9 is a potential candidate for further development of tyrosinase inhibitors.en_US
dc.subjectBiochemistry, Genetics and Molecular Biologyen_US
dc.subjectPharmacology, Toxicology and Pharmaceuticsen_US
dc.titleMethoxy-substituted tyramine derivatives synthesis, computational studies and tyrosinase inhibitory kineticsen_US
article.volume26en_US of Gujraten_US Iqbal Open Universityen_US Mai Universityen_US of Bahrainen_US
Appears in Collections:CMUL: Journal Articles

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