Smoothened Antagonists for Hair Inhibition

    August 2010 in “ Bioorganic & medicinal chemistry letters ”
    Jie Jack Li, Veerabahu Shanmugasundaram, Satya L. Reddy, Laura Fleischer, Zenquan Wang, Yvonne Smith, William G. Harter, Wen-Song Yue, Manju Swaroop, Ling Li, Christy Xiaodong Ji, Danielle Dettling, Bella Osak, Laura Rydelek Fitzgerald, Robert A. Conradi
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    TLDR Two new compounds were found to effectively reduce hair growth in mice.
    In the study from 2010, researchers synthesized a series of aminomethylpyrazoles and tested them for their ability to inhibit the Smoothened (Smo) pathway, which is involved in hair growth. Two compounds, 10k and 10l, demonstrated potent Smo antagonism and were effective in suppressing hair growth in the C3H/HeN mouse model. Compound 10l, which was more selective, also showed a low risk of causing photo-irritation as it tested negative in the 3T3 NRU assay. Although 10l was slightly less effective than the reference compound eflornithine, it was still efficacious in reducing hair growth in mice.
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