2. Academic Validation
  3. Smoothened antagonists for hair inhibition

Smoothened antagonists for hair inhibition

  • Bioorg Med Chem Lett. 2010 Aug 15;20(16):4932-5. doi: 10.1016/j.bmcl.2010.06.033.
Jie Jack Li 1,  Veerabahu Shanmugasundaram,  Satya Reddy,  Laura L Fleischer,  Zenquan Wang,  Yvonne Smith,  William G Harter,  Wen-Song Yue,  Manju Swaroop,  Ling Li,  Christy Xiaodong Ji,  Danielle Dettling,  Bella Osak,  Laura R Fitzgerald,  Robert Conradi
Affiliations

Affiliation

  • 1 Department of Chemistry, Michigan Laboratories, Pfizer Global Research & Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. jack.li@bms.com
PMID: 20620058 DOI: 10.1016/j.bmcl.2010.06.033
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).

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