期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 16, 页码 4932-4935出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.033
关键词
Smoothened antagonists; Hair; Photo-irritation; Aminomethylpyrazoles
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). (c) 2010 Elsevier Ltd. All rights reserved.
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