Zhou, Y.; Li, Q.; Fu, R.; Yang, H.; Mo, J.; Chen, Y.; Xia, Q. Synthesis and Structure-Activity Relationships of Resorcinol Derivatives as Highly Potent Tyrosinase Inhibitors. Preprints2018, 2018110330. https://doi.org/10.20944/preprints201811.0330.v1
APA Style
Zhou, Y., Li, Q., Fu, R., Yang, H., Mo, J., Chen, Y., & Xia, Q. (2018). Synthesis and Structure-Activity Relationships of Resorcinol Derivatives as Highly Potent Tyrosinase Inhibitors. Preprints. https://doi.org/10.20944/preprints201811.0330.v1
Chicago/Turabian Style
Zhou, Y., Yao Chen and Qingyou Xia. 2018 "Synthesis and Structure-Activity Relationships of Resorcinol Derivatives as Highly Potent Tyrosinase Inhibitors" Preprints. https://doi.org/10.20944/preprints201811.0330.v1
Abstract
Compounds with tyrosinase inhibitory efficacy could be effective as depigmenting agents. Although a large number of natural and synthetic tyrosinase inhibitors have been reported, few of them are used as skin-whitening agents due to poor activity and safety concerns. 3-(2,4-Dihydroxyphenyl)propionic acid (DPPA), a naturally occurring compound isolated from Ficus carica, was previously discovered as a moderate tyrosinase inhibitor. In this study, the structure-activity relationship study of DPPA was conducted. Compound 3g, with the 2,4-resorcinol subunit and terminal hydrophobic di-butylamino group, was identified with low nanomolar enzymatic IC50 value. Additionally, compound 3g could effectively reduce melanin levels in B16-F10 melanoma cells treated with α-melanocyte-stimulating hormone (α-MSH) without affecting cell viability and proliferation. All these results indicated that compound 3g could be considered as a promising candidate for the treatment of diseases associated with hyperpigmentation.
Chemistry and Materials Science, Medicinal Chemistry
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