1246639-95-1Relevant academic research and scientific papers
Development of autotaxin inhibitors: A series of zinc binding triazoles
Thomson, Christopher G.,Le Grand, Darren,Dowling, Mark,Brocklehurst, Cara E.,Chinn, Colin,Elphick, Lucy,Faller, Michael,Freeman, Mark,Furminger, Vikki,Gasser, Cornelia,Hamadi, Ahmed,Hardaker, Elizabeth,Head, Victoria,Hill, Johan C.,Janus, Diana I.,Pearce, David,Poulaud, Anne-Sophie,Stanley, Emily,Sviridenko, Lilya
, p. 2279 - 2284 (2018/05/24)
A series of inhibitors of Autotaxin (ATX) has been developed using the binding mode of known inhibitor, PF-8380, as a template. Replacement of the benzoxazolone with a triazole zinc-binding motif reduced crystallinity and improved solubility relative to PF-8380. Modification of the linker region removed hERG activity and led to compound 12 – a selective, high affinity, orally-bioavailable inhibitor of ATX. Compound 12 concentration-dependently inhibits autotaxin and formation of LPA in vivo, as shown in pharmacokinetic-pharmacodynamic experiments.
HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS
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Page/Page column 20, (2012/02/01)
Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.
