Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
Raynaud, Florence I, Eccles, Suzanne A, Patel, Sonal, Alix, Sonia, Box, Gary, Chuckowree, Irina, Folkes, Adrian, Gowan, Sharon, De Haven Brandon, Alexis, Di Stefano, Francesca, Hayes, Angela, Henley, Alan T, Lensun, Letitia, Pergl-Wilson, Giles, Robson, Anthony, Saghir, Nahid, Zhyvoloup, Alexander, McDonald, Edward, Sheldrake, Peter, Shuttleworth, Stephen, Valenti, Melanie, Wan, Nan Chi, Clarke, Paul A, Workman, Paul
Published in Molecular cancer therapeutics (01.07.2009)
Published in Molecular cancer therapeutics (01.07.2009)
Get full text
Journal Article
Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform
Heffron, Timothy P, Wei, BinQing, Olivero, Alan, Staben, Steven T, Tsui, Vickie, Do, Steven, Dotson, Jennafer, Folkes, Adrian J, Goldsmith, Paul, Goldsmith, Richard, Gunzner, Janet, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Shuttleworth, Stephen, Sutherlin, Daniel P, Wan, Nan Chi, Wang, Shumei, Wiesmann, Christian, Zhu, Bing-Yan
Published in Journal of medicinal chemistry (24.11.2011)
Published in Journal of medicinal chemistry (24.11.2011)
Get full text
Journal Article
Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer
Sutherlin, Daniel P, Sampath, Deepak, Berry, Megan, Castanedo, Georgette, Chang, Zhigang, Chuckowree, Irina, Dotson, Jenna, Folkes, Adrian, Friedman, Lori, Goldsmith, Richard, Heffron, Tim, Lee, Leslie, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Olivero, Alan, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Tian, Qingping, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wiesmann, Christian, Wong, Susan, Zhu, Bing-Yan
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
Get full text
Journal Article
The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer
Folkes, Adrian J, Ahmadi, Khatereh, Alderton, Wendy K, Alix, Sonia, Baker, Stewart J, Box, Gary, Chuckowree, Irina S, Clarke, Paul A, Depledge, Paul, Eccles, Suzanne A, Friedman, Lori S, Hayes, Angela, Hancox, Timothy C, Kugendradas, Arumugam, Lensun, Letitia, Moore, Pauline, Olivero, Alan G, Pang, Jodie, Patel, Sonal, Pergl-Wilson, Giles H, Raynaud, Florence I, Robson, Anthony, Saghir, Nahid, Salphati, Laurent, Sohal, Sukhjit, Ultsch, Mark H, Valenti, Melanie, Wallweber, Heidi J.A, Wan, Nan Chi, Wiesmann, Christian, Workman, Paul, Zhyvoloup, Alexander, Zvelebil, Marketa J, Shuttleworth, Stephen J
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
Get full text
Journal Article
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor
Heffron, Timothy P., Berry, Megan, Castanedo, Georgette, Chang, Christine, Chuckowree, Irina, Dotson, Jennafer, Folkes, Adrian, Gunzner, Janet, Lesnick, John D., Lewis, Cristina, Mathieu, Simon, Nonomiya, Jim, Olivero, Alan, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steve, Sutherlin, Daniel P., Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wong, Susan, Zhu, Bing-yan
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Get full text
Journal Article
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
Staben, Steven T., Heffron, Timothy P., Sutherlin, Daniel P., Bhat, Seema R., Castanedo, Georgette M., Chuckowree, Irina S., Dotson, Jenna, Folkes, Adrian J., Friedman, Lori S., Lee, Leslie, Lesnick, John, Lewis, Cristina, Murray, Jeremy M., Nonomiya, Jim, Olivero, Alan G., Plise, Emile, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Rouge, Lionel, Sampath, Deepak, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Weismann, Christian, Wu, Ping, Zhu, Bing-Yan
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Get full text
Journal Article
Novel Angular Benzophenazines: Dual Topoisomerase I and Topoisomerase II Inhibitors as Potential Anticancer Agents
Vicker, Nigel, Burgess, Luke, Chuckowree, Irina S, Dodd, Rory, Folkes, Adrian J, Hardick, David J, Hancox, Timothy C, Miller, Warren, Milton, John, Sohal, Sukhjit, Wang, Shouming, Wren, Stephen P, Charlton, Peter A, Dangerfield, Wendy, Liddle, Chris, Mistry, Prakash, Stewart, Alistair J, Denny, William A
Published in Journal of medicinal chemistry (31.01.2002)
Published in Journal of medicinal chemistry (31.01.2002)
Get full text
Journal Article
Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1
Folkes, Adrian, Roe, Michael B, Sohal, Sukhjit, Golec, Julian, Faint, Richard, Brooks, Teresa, Charlton, Peter
Published in Bioorganic & medicinal chemistry letters (08.10.2001)
Published in Bioorganic & medicinal chemistry letters (08.10.2001)
Get full text
Journal Article
Abstract C201: A novel potent and selective inhibitor of PI3K/mTOR, GDC-0980, currently in phase I clinical trials
Friedman, Lori S., Belvin, Marcia, Berry, Leanne, Berry, Megan, Castanedo, Georgette, Edgar, Kyle, Folkes, Adrian, Guan, Jane, Heffron, Tim, Lesnick, John, Lewis, Cris, Nonomiya, Jim, Olivero, Alan, Patel, Sonal, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Sampath, Deepak, Sutherlin, Dan, Wallin, Jeff, Zhu, Bingyan
Published in Molecular cancer therapeutics (10.12.2009)
Published in Molecular cancer therapeutics (10.12.2009)
Get full text
Journal Article
Novel Inhibitors of Plasminogen Activator Inhibitor-1: Development of New Templates From Diketopiperazines
Wang, Shouming, Golec, Julian, Miller, Warren, Milutinovic, Sandra, Folkes, Adrian, Williams, Susannah, Brooks, Teresa, Hardman, Kevin, Charlton, Peter, Wren, Stephen, Spencer, John
Published in Bioorganic & medicinal chemistry letters (02.09.2002)
Published in Bioorganic & medicinal chemistry letters (02.09.2002)
Get full text
Journal Article
Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1
FOLKES, Adrian, BROWN, S. David, LEAHY, James W, MACH, Morrison, MATTHEWS, David, PRISBYLLA, Michael P, SANDERSON, Jason, SIMON, Reyna J, TESFAI, Zerom, VICKER, Nigel, WANG, Shouming, WEBB, Robert R, CANNE, Lynne E, CHARLTON, Peter, CHAN, Jocelyn, ENGELHARDT, Erin, EPSHTEYN, Sergey, FAINT, Richard, GOLEC, Julian, HANEL, Art, KEARNEY, Patrick
Published in Bioorganic & medicinal chemistry letters (08.04.2002)
Published in Bioorganic & medicinal chemistry letters (08.04.2002)
Get full text
Journal Article
Studies on Pyrrolopyrimidines as Selective Inhibitors of Multidrug-Resistance- Associated Protein in Multidrug Resistance
Wang, Shouming, Folkes, Adrian, Chuckowree, Irina, Cockcroft, Xiaoling, Sohal, Sukhjit, Miller, Warren, Milton, John, Wren, Stephen P, Vicker, Nigel, Depledge, Paul, Scott, John, Smith, Lyndsay, Jones, Hazel, Mistry, Prakash, Faint, Richard, Thompson, Deanne, Cocks, Simon
Published in Journal of medicinal chemistry (11.03.2004)
Published in Journal of medicinal chemistry (11.03.2004)
Get full text
Journal Article
Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors
Olivero, Alan G., Heffron, Timothy P., Baumgardner, Matthew, Belvin, Marcia, Ross, Leanne Berry, Blaquiere, Nicole, Bradley, Erin, Castanedo, Georgette, Derynck, Mika, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle, Folkes, Adrian, Francis, Ross, Gianetti, Tony, Goldsmith, Richard, Goldsmith, Paul, Guan, Jane, Harrison, Trevor, Heald, Robert, Hsu, Jerry, Jackson, Phillip, Jones, Graham, Kim, Amy, Kolesnikov, Aleks, Lackner, Mark, Lee, Leslie, Lesnick, John, Lewis, Cristina, Mamounas, Michael, McLean, Neville, Murray, Jeremy, Ndubaku, Chudi, Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Prior, Wei Wei, Salphati, Laurent, Sampath, Deepack, Sideris, Stephen, Siu, Michael, Staben, Steven, Sutherlin, Daniel, Ultsch, Mark, Wallin, Jeff, Wang, Lan, Wiesmann, Christian, Zhang, Xiaolin, Friedman, Lori S.
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Get full text
Journal Article
Abstract 2787: Discovery of GDC-0980, a selective PI3K/mTOR inhibitor in clinical trials
Sutherlin, Daniel P., Belvin, Marcia, Bao, Linda, Berry, Leanne, Berry, Megan, Castanedo, Georgette, Edgar, Kyle, Folkes, Adrian, Friedman, Lori, Heffron, Tim, Patel, Sonal, Olivero, Alan, Lesnick, John, Lewis, Cristina, Marsters, James, Nonomiya, Jim, Pang, Jodie, Prior, Wei Wei, Salphati, Laurent, Sampath, Deepak, Tsui, Vickie, Wallin, Jeff, Wei, BinQing, Weismann, Christian, Zhu, Bing-Yan
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Published in Cancer research (Chicago, Ill.) (15.04.2011)
Get full text
Journal Article
Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives
Roe, Michael, Folkes, Adrian, Ashworth, Philip, Brumwell, Julie, Chima, Lal, Hunjan, Sukhjit, Pretswell, Ian, Dangerfield, Wendy, Ryder, Hamish, Charlton, Peter
Published in Bioorganic & medicinal chemistry letters (22.02.1999)
Published in Bioorganic & medicinal chemistry letters (22.02.1999)
Get full text
Journal Article
Design and Synthesis of New Templates Derived from Pyrrolopyrimidine as Selective Multidrug-Resistance-Associated Protein Inhibitors in Multidrug Resistance
Wang, Shouming, Wan, Nan Chi, Harrison, John, Miller, Warren, Chuckowree, Irina, Sohal, Sukhjit, Hancox, Timothy C, Baker, Stewart, Folkes, Adrian, Wilson, Francis, Thompson, Deanne, Cocks, Simon, Farmer, Hayley, Boyce, Anthony, Freathy, Caroline, Broadbridge, Jan, Scott, John, Depledge, Paul, Faint, Richard, Mistry, Prakash, Charlton, Peter
Published in Journal of medicinal chemistry (11.03.2004)
Published in Journal of medicinal chemistry (11.03.2004)
Get full text
Journal Article
PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
SUTHERLIN DANIEL P, FOLKES ADRIAN, WAN NAN CHI, CASTANEDO GEORGETTE, CHUCKOWREE IRINA
Year of Publication 25.04.2011
Get full text
Year of Publication 25.04.2011
Patent
PHARMACEUTICAL COMPOUNDS
LATIF MOHAMMED A, CHUCKOWREE IRINA S, HANCOX TIMOTHY C, SOHAL SUKHJIT, BAKER STEWART J, FOLKES ADRIAN J, WAN NAN CHI, SHUTTLEWORTH STEPHEN J
Year of Publication 19.06.2013
Get full text
Year of Publication 19.06.2013
Patent
BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
GOLDSMITH RICHARD A, WEI BINQING, NDUBAKU CHUDI, BLAQUIERE NICOLE, KOLESNIKOV ALEKSANDR, DUDLEY DANETTE, DO STEVEN, OLIVERO ALAN G, PRICE STEPHEN, STABEN STEVEN, FOLKES ADRIAN J, HEFFRON TIM, HEALD ROBERT
Year of Publication 20.03.2014
Get full text
Year of Publication 20.03.2014
Patent