| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10587679 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
Removal of the basic piperazine nitrogen atom, introduction of a solubilising end group and partial reduction of the triazolopyridazine moiety in the previously-described lead androgen receptor downregulator 1 addressed hERG and physical property issues and led to clinical candidate AZD3514 (12), that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert H. Bradbury, David G. Acton, Nicola L. Broadbent, A. Nigel Brooks, Gregory R. Carr, Glenn Hatter, Barry R. Hayter, Kathryn J. Hill, Nicholas J. Howe, Rhys D.O. Jones, David Jude, Scott G. Lamont, Sarah A. Loddick, Heather L. McFarland,