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■ Identification, Synthesis and Photo-Protection Evaluation of Arylthiazole Derivatives as a Novel Series of Sunscreens

Guoliang Li, Yundong He, Wenbo Zhou, Peng Wang, Yong Zhang, Weiguang Tong, Haigang Wu, Mingyao Liu, Xiyun Ye,* and Yihua Chen*

*Institute of Biomedical Sciences and School of Life Sciences, Shanghai Key Laboratory of Regulatory Biology, East China Normal University, 500 Dongchuan Rd., Minhang, Shanghai 200241, China

Abstract

A novel series of aryl thiazole derivatives have been designed, synthesized and evaluated in preventing keratinocyte cell (HaCaT) from UVB exposure induced cellar damage. The structure-activity relationship (SAR) was discussed from chemical modification of amide, aryl-thiazole rings and the linker. Preliminary data suggested that four compounds (5a, 11a, 13c and 17) effectively protected Keratinocytes cell from UVB induced cell death compare with positive control polydatin. More importantly, compound 5a significantly protected the dorsal skin of BALB/c-nu mice against UVB-induced decrustation in vivo. The in vitro and in vivo data for these aryl thiazole derivatives suggest further studies for their potential use as photo-protection agents as well as sunscreen candidates.