Search Results - "Davey, Paul R. J"

Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist by Scott, James S, Moss, Thomas A, Balazs, Amber, Barlaam, Bernard, Breed, Jason, Carbajo, Rodrigo J, Chiarparin, Elisabetta, Davey, Paul R. J, Delpuech, Oona, Fawell, Stephen, Fisher, David I, Gagrica, Sladjana, Gangl, Eric T, Grebe, Tyler, Greenwood, Ryan D, Hande, Sudhir, Hatoum-Mokdad, Holia, Herlihy, Kara, Hughes, Samantha, Hunt, Thomas A, Huynh, Hoan, Janbon, Sophie L. M, Johnson, Tony, Kavanagh, Stefan, Klinowska, Teresa, Lawson, Mandy, Lister, Andrew S, Marden, Stacey, McGinnity, Dermot F, Morrow, Christopher J, Nissink, J. Willem M, O’Donovan, Daniel H, Peng, Bo, Polanski, Radoslaw, Stead, Darren S, Stokes, Stephen, Thakur, Kumar, Throner, Scott R, Tucker, Michael J, Varnes, Jeffrey, Wang, Haixia, Wilson, David M, Wu, Dedong, Wu, Ye, Yang, Bin, Yang, Wenzhan

“…Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER+…”
Get full text

Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models by Winter-Holt, Jon J, Bardelle, Catherine, Chiarparin, Elisabetta, Dale, Ian L, Davey, Paul R. J, Davies, Nichola L, Denz, Christopher, Fillery, Shaun M, Guérot, Carine M, Han, Fujin, Hughes, Samantha J, Kulkarni, Meghana, Liu, Zhaoqun, Milbradt, Alexander, Moss, Thomas A, Niu, Huijun, Patel, Joe, Rabow, Alfred A, Schimpl, Marianne, Shi, Junjie, Sun, Dongqing, Yang, Dejian, Guichard, Sylvie

“…ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While…”
Get full text

Characterization of the Kinetic Mechanism of Human Protein Arginine Methyltransferase 5 by Eddershaw, Alice R, Stubbs, Christopher J, Edwardes, Lucy V, Underwood, Elizabeth, Hamm, Gregory R, Davey, Paul R. J, Clarkson, Paul N, Syson, Karl

“…Protein arginine methyltransferases (PRMTs) are of great interest for the development of therapeutics due to their involvement in a number of malignancies,…”
Get full text

Tricyclic IndazolesA Novel Class of Selective Estrogen Receptor Degrader Antagonists by Scott, James S, Bailey, Andrew, Buttar, David, Carbajo, Rodrigo J, Curwen, Jon, Davey, Paul R. J, Davies, Robert D. M, Degorce, Sébastien L, Donald, Craig, Gangl, Eric, Greenwood, Ryan, Groombridge, Sam D, Johnson, Tony, Lamont, Scott, Lawson, Mandy, Lister, Andrew, Morrow, Christopher J, Moss, Thomas A, Pink, Jennifer H, Polanski, Radoslaw

“…Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists…”
Get full text

Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833 by Scott, James S, Moss, Thomas A, Barlaam, Bernard, Davey, Paul R. J, Fairley, Gary, Gangl, Eric T, Greenwood, Ryan D. R, Hatoum-Mokdad, Holia, Lister, Andrew S, Longmire, David, Polanski, Radoslaw, Stokes, Stephen, Tucker, Michael J, Varnes, Jeffrey G, Yang, Bin

“…Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of…”
Get full text

Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling by Wendt, Mathias, Bellavita, Rosa, Gerber, Alan, Efrém, Nina‐Louisa, Ramshorst, Thirza, Pearce, Nicholas M., Davey, Paul R. J., Everard, Isabel, Vazquez‐Chantada, Mercedes, Chiarparin, Elisabetta, Grieco, Paolo, Hennig, Sven, Grossmann, Tom N.

“…Protein complexes are defined by the three‐dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design…”
Get full text

Design, Synthesis, and Analytical Evaluation of Fsp3‐Inspired Raman Probes for Cellular Imaging by Steven, Craig F., Lee, Martin, Nichol, Gary S., Davey, Paul R. J., Chiarparin, Elisabetta, Brunton, Valerie G., Hulme, Alison N.

“…The fraction of sp3‐hybdrised carbons (Fsp3) in drug candidates and other biologically relevant compounds has been proposed to be an important physicochemical…”
Get full text

Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists by Scott, James S., Stead, Darren, Barlaam, Bernard, Breed, Jason, Carbajo, Rodrigo J., Chiarparin, Elisabetta, Cureton, Natalie, Davey, Paul R. J., Fisher, David I., Gangl, Eric T., Grebe, Tyler, Greenwood, Ryan D., Hande, Sudhir, Hatoum-Mokdad, Holia, Hughes, Samantha J., Hunt, Thomas A., Johnson, Tony, Kavanagh, Stefan L., Klinowska, Teresa C. M., Larner, Carrie J. B., Lawson, Mandy, Lister, Andrew S., Longmire, David, Marden, Stacey, McGuire, Thomas M., McMillan, Caroline, McMurray, Lindsay, Morrow, Christopher J., Nissink, J. Willem M., Moss, Thomas A., O’Donovan, Daniel H., Polanski, Radoslaw, Stokes, Stephen, Thakur, Kumar, Trueman, Dawn, Truman, Caroline, Tucker, Michael J., Wang, Haixia, Whalley, Nicky, Wu, Dedong, Wu, Ye, Yang, Bin, Yang, Wenzhan

“…Herein, we report the optimization of a meta-substituted series of selective estrogen receptor degrader (SERD) antagonists for the treatment of ER+ breast…”
Get full text

Rücktitelbild: Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling (Angew. Chem. 25/2021) by Wendt, Mathias, Bellavita, Rosa, Gerber, Alan, Efrém, Nina‐Louisa, Ramshorst, Thirza, Pearce, Nicholas M., Davey, Paul R. J., Everard, Isabel, Vazquez‐Chantada, Mercedes, Chiarparin, Elisabetta, Grieco, Paolo, Hennig, Sven, Grossmann, Tom N.

“…Bizyklische Peptidomimetika binden den transkriptionellen Coaktivator β‐Catenin. Eine strukturbasierte Designstrategie wurde angewandt, um ein 52 Aminosäuren…”
Get full text

Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling by Wendt, Mathias, Bellavita, Rosa, Gerber, Alan, Efrém, Nina‐Louisa, Ramshorst, Thirza, Pearce, Nicholas M., Davey, Paul R. J., Everard, Isabel, Vazquez‐Chantada, Mercedes, Chiarparin, Elisabetta, Grieco, Paolo, Hennig, Sven, Grossmann, Tom N.

“…Protein complexes are defined by the three‐dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design…”
Get full text

Facile preparation and Suzuki–Miyaura cross-coupling of N-2-alkylated 2H-1,2,3-triazole 4-boronates by Davey, Paul R.J., Delouvrié, Bénédicte, Dorison-Duval, Delphine, Germain, Hervé, Harris, Craig S., Magnien, Françoise, Ouvry, Gilles, Tricotet, Thomas

“…The preparation of N-2 substituted 2H-1,2,3-triazoles substituted at C-4 with an organometallic moiety has no recognised precedent. Herein, we report their…”
Get full text

Design, Synthesis, and Analytical Evaluation of Fsp 3 ‐Inspired Raman Probes for Cellular Imaging by Steven, Craig F., Lee, Martin, Nichol, Gary S., Davey, Paul R. J., Chiarparin, Elisabetta, Brunton, Valerie G., Hulme, Alison N.

“…Abstract The fraction of sp 3 ‐hybdrised carbons (Fsp 3 ) in drug candidates and other biologically relevant compounds has been proposed to be an important…”
Get full text

Back Cover: Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling (Angew. Chem. Int. Ed. 25/2021) by Wendt, Mathias, Bellavita, Rosa, Gerber, Alan, Efrém, Nina‐Louisa, Ramshorst, Thirza, Pearce, Nicholas M., Davey, Paul R. J., Everard, Isabel, Vazquez‐Chantada, Mercedes, Chiarparin, Elisabetta, Grieco, Paolo, Hennig, Sven, Grossmann, Tom N.

“…Bicyclic peptidomimetics bind the transcriptional coactivator β‐catenin. A structure‐based design strategy has been applied to minimize a 52 amino acid binding…”
Get full text

Facile, diversity-orientated one-pot synthesis of ethyl 1,5-disubstituted-1H-1,2,4-triazole-3-carboxylates by Degorce, Sébastien, Delouvrié, Bénédicte, Davey, Paul R.J., Didelot, Myriam, Germain, Hervé, Harris, Craig S., Brempt, Christine Lambert-van der, Lebraud, Honorine, Ouvry, Gilles

“…Access to the 1,5-disubstituted-1H-1,2,4-triazole-3-carboxamide motif is quite laborious and requires forcing conditions to effect the cyclocondensation step…”
Get full text