Search Results - "Mortlock, Andrew A."

AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis by WILKINSON, Robert W, ODEDRA, Rajesh, BYTH, Kate F, BARRASS, Nigel C, MUNDT, Kirsten E, FOOTE, Kevin M, HERON, Nicola M, JUNG, Frederic H, MORTLOCK, Andrew A, BOYLE, F. Thomas, GREEN, Stephen, HEATON, Simon P, WEDGE, Stephen R, KEEN, Nicholas J, CRAFTER, Claire, FOSTER, John R, BRADY, Madeleine C, BIGLEY, Alison, BROWN, Elaine

“…Purpose: In the current study, we examined the in vivo effects of AZD1152, a novel and specific inhibitor of Aurora kinase activity (with selectivity for…”
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Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase by Mortlock, Andrew A, Foote, Kevin M, Heron, Nicola M, Jung, Frédéric H, Pasquet, Georges, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, De Savi, Chris, Roberts, Nicola J, Johnson, Trevor, Dousson, Cyril B, Hill, George B, Perkins, David, Hatter, Glenn, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Crafter, Claire, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen, Khatri, Liz, Brady, Madeleine C, Kearney, Sarah, McKillop, David, Rhead, Steve, Parry, Tony, Green, Stephen

“…The Aurora kinases have been the subject of considerable interest as targets for the development of new anticancer agents. While evidence suggests inhibition…”
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SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors by Heron, Nicola M., Anderson, Malcolm, Blowers, David P., Breed, Jason, Eden, Jonathan M., Green, Stephen, Hill, George B., Johnson, Trevor, Jung, Frederic H., McMiken, Helen H.J., Mortlock, Andrew A., Pannifer, Andrew D., Pauptit, Richard A., Pink, Jennifer, Roberts, Nicola J., Rowsell, Siân

“…The discovery, optimisation and subsequent structural determination of a novel class of Aurora kinase inhibitors are described. A novel series of…”
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Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer by 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.

“…As an approach to treatment of advanced prostate cancer, a medicinal chemistry program derived from a novel androgen receptor ligand 8a led to androgen…”
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Discovery of Novel and Potent Thiazoloquinazolines as Selective Aurora A and B Kinase Inhibitors by Jung, Frédéric H, Pasquet, Georges, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, Germain, Hervé, De Savi, Chris, Roberts, Nicola, Johnson, Trevor, Dousson, Cyril, Hill, George B, Mortlock, Andrew A, Heron, Nicola, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Green, Stephen, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen

“…The synthesis of a novel series of quinazolines substituted at C4 by five-membered ring aminoheterocycles is reported. Their in vitro structure−activity…”
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Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: Selective inhibitors of Aurora B kinase with potent anti-tumor activity by Foote, Kevin M., Mortlock, Andrew A., Heron, Nicola M., Jung, Frédéric H., Hill, George B., Pasquet, Georges, Brady, Madeleine C., Green, Stephen, Heaton, Simon P., Kearney, Sarah, Keen, Nicholas J., Odedra, Rajesh, Wedge, Stephen R., Wilkinson, Robert W.

“…A new class of 1-acetanilide-4-aminopyrazole-substituted quinazoline Aurora kinase inhibitors has been discovered possessing highly potent cellular activity…”
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Total Syntheses of (−)-Papuamine and (−)-Haliclonadiamine by McDermott, Todd S, Mortlock, Andrew A, Heathcock, Clayton H

“…The pentacyclic marine alkaloids (−)-papuamine (1) and (−)-haliclonadiamine (2) have been prepared by total synthesis. The synthesis began with (−)-8, which…”
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Structure–activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 1 by Delouvrié, Bénédicte, Al-Kadhimi, Katherine, Arnould, Jean-Claude, Barry, Simon T., Cross, Darren A.E., Didelot, Myriam, Gavine, Paul R., Germain, Hervé, Harris, Craig S., Hughes, Adina M., Jude, David A., Kendrew, Jane, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Ménard, Morgan, Mortlock, Andrew A., Pass, Martin, Rooney, Claire, Vautier, Michel, Vincent, Jennifer L., Warin, Nicolas

“…Potent antagonists of the integrin α5β1, which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency…”
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Structure–activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 2 by Delouvrié, Bénédicte, Al-Kadhimi, Katherine, Arnould, Jean-Claude, Barry, Simon T., Cross, Darren A.E., Didelot, Myriam, Gavine, Paul R., Germain, Hervé, Harris, Craig S., Hughes, Adina M., Jude, David A., Kendrew, Jane, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Ménard, Morgan, Mortlock, Andrew A., Pass, Martin, Rooney, Claire, Vautier, Michel, Vincent, Jennifer L., Warin, Nicolas

“…Potent antagonists of the integrin α5β1, which are RGD mimetics built from tyrosine are described. This paper describes the optimization of in vitro potency…”
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Progress in the development of selective inhibitors of aurora kinases by Mortlock, Andrew A, Keen, Nicholas J, Jung, Frederic H, Heron, Nicola M, Foote, Kevin M, Wilkinson, Robert W, Green, Stephen

“…Errors in the mitotic process are thought to be one of the principal sources of the genetic instability that hallmarks cancer. Unsurprisingly, many of the…”
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New Non-Peptide Endothelin-A Receptor Antagonists:  Synthesis, Biological Properties, and Structure−Activity Relationships of 5-(Dimethylamino)-N-pyridyl-, -N-pyrimidinyl-, -N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides by Bradbury, Robert H, Bath, Colin, Butlin, Roger J, Dennis, Michael, Heys, Christine, Hunt, Sarah J, James, Roger, Mortlock, Andrew A, Sumner, Neil F, Tang, Eric K, Telford, Berwick, Whiting, Elaine, Wilson, Campbell

“…Use of automated synthesis led to the discovery of several 6-membered nitrogen heterocycles as replacements for the N-isoxazolyl substituent present in the…”
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Structureaactivity relationship of a series of non peptidic RGD integrin antagonists targeting I-5I21: Part 2 by Delouvrie, Benedicte, Al-Kadhimi, Katherine, Arnould, Jean-Claude, Barry, Simon T, Cross, Darren AE, Didelot, Myriam, Gavine, Paul R, Germain, Herve, Harris, Craig S, Hughes, Adina M, Jude, David A, Kendrew, Jane, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Menard, Morgan, Mortlock, Andrew A, Pass, Martin, Rooney, Claire, Vautier, Michel, Vincent, Jennifer L, Warin, Nicolas

“…Potent antagonists of the integrin I-5I21, which are RGD mimetics built from tyrosine are described. This paper describes the optimization of in vitro potency…”
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Structureaactivity relationship of a series of non peptidic RGD integrin antagonists targeting I-5I21: Part 1 by Delouvrie, Benedicte, Al-Kadhimi, Katherine, Arnould, Jean-Claude, Barry, Simon T, Cross, Darren AE, Didelot, Myriam, Gavine, Paul R, Germain, Herve, Harris, Craig S, Hughes, Adina M, Jude, David A, Kendrew, Jane, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Menard, Morgan, Mortlock, Andrew A, Pass, Martin, Rooney, Claire, Vautier, Michel, Vincent, Jennifer L, Warin, Nicolas

“…Potent antagonists of the integrin I-5I21, which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency…”
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N-methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide ; One of a class of novel benzenesulphonamides which are orally-active, ETA-Selective endothelin antagonists by MORTLOCK, A. A, BATH, C, WRIGHT, N. D, BUTLIN, R. J, HEYS, C, HUNT, S. J, REID, A. C, SUMNER, N. F, TANG, E. K, WHITING, E, WILSON, C

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Approaches to the γ-lactone unit of CP-225,917 and CP-263,114 by Armstrong, Alan, Critchley, Trevor J., Gourdel-Martin, Marie-Edith, Kelsey, Richard D., Mortlock, Andrew A.

“…Synthesis of the γ-lactone unit of CP-225,917 and CP-263,114 is reported by differentiation of a diester at C14 using either selective monohydrolysis or…”
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SARr and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors by HERON, Nicola M, ANDERSON, Malcolm, MORTLOCK, Andrew A, PANNIFER, Andrew D, PAUPTIT, Richard A, PINK, Jennifer, ROBERTS, Nicola J, ROWSELL, Sian, BLOWERS, David P, BREED, Jason, EDEN, Jonathan M, GREEN, Stephen, HILL, George B, JOHNSON, Trevor, JUNG, Frederic H, MCMIKEN, Helen H. J

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N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; one of a class of novel benzenesulphonamides which are orally-active, ET A-selective endothelin antagonists by Mortlock, Andrew A., Bath, Colin, Butlin, Roger J., Heys, Christine, Hunt, Sarah J., Reid, Alan C., Sumner, Neil F., Tang, Eric K., Whiting, Elaine, Wilson, Campbell, Wright, Nicola D.

“…A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ET A receptor…”
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