338748-56-4Relevant academic research and scientific papers
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer
Bradbury, Robert H.,Acton, David G.,Broadbent, Nicola L.,Brooks, A. Nigel,Carr, Gregory R.,Hatter, Glenn,Hayter, Barry R.,Hill, Kathryn J.,Howe, Nicholas J.,Jones, Rhys D.O.,Jude, David,Lamont, Scott G.,Loddick, Sarah A.,McFarland, Heather L.,Parveen, Zaieda,Rabow, Alfred A.,Sharma-Singh, Gorkhn,Stratton, Natalie C.,Thomason, Andrew G.,Trueman, Dawn,Walker, Graeme E.,Wells, Stuart L.,Wilson, Joanne,Wood, J. Matthew
supporting information, p. 1945 - 1948 (2013/05/09)
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 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b] pyridazine (1) addressed hERG and physical property issues, and led to clinical candidate 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3- (trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.
Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer
Bradbury, Robert H.,Hales, Neil J.,Rabow, Alfred A.,Walker, Graeme E.,Acton, David G.,Andrews, David M.,Ballard, Peter,Brooks, Nigel A.N.,Colclough, Nicola,Girdwood, Alan,Hancox, Urs J.,Jones, Owen,Jude, David,Loddick, Sarah A.,Mortlock, Andrew A.
scheme or table, p. 5442 - 5445 (2011/10/12)
Chemical starting points were investigated for downregulation of the androgen receptor as an approach to treatment of advanced prostate cancer. Although prototypic steroidal downregulators such as 6a designed for intramuscular administration showed insuff
