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ID: ALA1208761
Journal: Bioorg Med Chem Lett
Title: Smoothened antagonists for hair inhibition.
Authors: Li JJ, Shanmugasundaram V, Reddy S, Fleischer LL, Wang Z, Smith Y, Harter WG, Yue WS, Swaroop M, Li L, Ji CX, Dettling D, Osak B, Fitzgerald LR, Conradi R.
Abstract: A series of aminomethylpyrazoles were prepared and evaluated using cell-based Smoothened beta-lactamase reporter assay and Smoothened binding assay. Potent Smoothened antagonists 10k and 10l were found to inhibit hair growth in vivo in the C3H/HeN mouse hair growth model. The more selective compound 10l was tested negative in the 3T3 NRU assay, indicating a low risk for causing photo-irritation and was efficacious using the C3H/HeN mouse hair growth model although it was slightly less efficacious than that of the reference compound eflornithine (7).
CiteXplore: 20620058