Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Adrian Folkes"'
Autor:
Paul Workman, Paul A. Clarke, Nan Chi Wan, Melanie Valenti, Stephen Shuttleworth, Peter Sheldrake, Edward McDonald, Alexander Zhyvoloup, Nahid Saghir, Anthony Robson, Giles Pergl-Wilson, Letitia Lensun, Alan T. Henley, Angela Hayes, Francesca Di Stefano, Alexis De Haven Brandon, Sharon Gowan, Adrian Folkes, Irina Chuckowree, Gary Box, Sonia Alix, Sonal Patel, Suzanne A. Eccles, Florence I. Raynaud
The phosphatidylinositide 3-kinase pathway is frequently deregulated in human cancers and inhibitors offer considerable therapeutic potential. We previously described the promising tricyclic pyridofuropyrimidine lead and chemical tool compound PI-103
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::085970df8f01140213c017be9fe8aaa7
https://doi.org/10.1158/1535-7163.c.6532217
https://doi.org/10.1158/1535-7163.c.6532217
Autor:
Paul Workman, Paul A. Clarke, Nan Chi Wan, Melanie Valenti, Stephen Shuttleworth, Peter Sheldrake, Edward McDonald, Alexander Zhyvoloup, Nahid Saghir, Anthony Robson, Giles Pergl-Wilson, Letitia Lensun, Alan T. Henley, Angela Hayes, Francesca Di Stefano, Alexis De Haven Brandon, Sharon Gowan, Adrian Folkes, Irina Chuckowree, Gary Box, Sonia Alix, Sonal Patel, Suzanne A. Eccles, Florence I. Raynaud
Supplementary Figure 1 from 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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88b69a6d0bf7df52af3de6589e9ad5e0
https://doi.org/10.1158/1535-7163.22486067.v1
https://doi.org/10.1158/1535-7163.22486067.v1
Autor:
Paul Workman, Paul A. Clarke, Nan Chi Wan, Melanie Valenti, Stephen Shuttleworth, Peter Sheldrake, Edward McDonald, Alexander Zhyvoloup, Nahid Saghir, Anthony Robson, Giles Pergl-Wilson, Letitia Lensun, Alan T. Henley, Angela Hayes, Francesca Di Stefano, Alexis De Haven Brandon, Sharon Gowan, Adrian Folkes, Irina Chuckowree, Gary Box, Sonia Alix, Sonal Patel, Suzanne A. Eccles, Florence I. Raynaud
Supplementary Figure 3C from 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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01c866c66e69073421c00311e11a606c
https://doi.org/10.1158/1535-7163.22486061.v1
https://doi.org/10.1158/1535-7163.22486061.v1
Autor:
Paul Workman, Paul A. Clarke, Nan Chi Wan, Melanie Valenti, Stephen Shuttleworth, Peter Sheldrake, Edward McDonald, Alexander Zhyvoloup, Nahid Saghir, Anthony Robson, Giles Pergl-Wilson, Letitia Lensun, Alan T. Henley, Angela Hayes, Francesca Di Stefano, Alexis De Haven Brandon, Sharon Gowan, Adrian Folkes, Irina Chuckowree, Gary Box, Sonia Alix, Sonal Patel, Suzanne A. Eccles, Florence I. Raynaud
Supplementary Table 1 from 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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4af932823949bf9230e37a31da950e4b
https://doi.org/10.1158/1535-7163.22486052.v1
https://doi.org/10.1158/1535-7163.22486052.v1
Autor:
Paul Workman, Paul A. Clarke, Nan Chi Wan, Melanie Valenti, Stephen Shuttleworth, Peter Sheldrake, Edward McDonald, Alexander Zhyvoloup, Nahid Saghir, Anthony Robson, Giles Pergl-Wilson, Letitia Lensun, Alan T. Henley, Angela Hayes, Francesca Di Stefano, Alexis De Haven Brandon, Sharon Gowan, Adrian Folkes, Irina Chuckowree, Gary Box, Sonia Alix, Sonal Patel, Suzanne A. Eccles, Florence I. Raynaud
Supplementary Figure 2 from 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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e805e180fd509a9ec2ce653e2f2de8e
https://doi.org/10.1158/1535-7163.22486064
https://doi.org/10.1158/1535-7163.22486064
Autor:
Lori Friedman, Lionel Rouge, Daniel P. Sutherlin, Georgette Castanedo, Adrian Folkes, Nan Chi Wan, Wei Wei Prior, Shumei Wang, Emile Plise, Ping Wu, Seema R. Bhat, Cristina Lewis, Deepak Sampath, Jeremy Murray, Alan G. Olivero, Jim Nonomiya, Timothy P. Heffron, Leslie Lee, Laurent Salphati, Irina Chuckowree, Steven T. Staben, Vickie Tsui, Bing-Yan Zhu, Christian Weismann, Jenna Dotson, Jodie Pang, John Lesnick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6048-6051
Starting from HTS hit 1a, X-ray co-crystallization and molecular modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochemical properties. Compound
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f5dfb15d68c0d5ace550e093eca7d77
https://doi.org/10.1016/j.bmcl.2010.08.067
https://doi.org/10.1016/j.bmcl.2010.08.067
Autor:
Cristina Lewis, Nan Chi Wan, Jennafer Dotson, Janet L. Gunzner, Georgette Castanedo, Deepak Sampath, Laurent Salphati, Jim Nonomiya, John Lesnick, Susan Wong, Timothy P. Heffron, Christine Chang, Megan Berry, Shumei Wang, Simon Mathieu, Jodie Pang, Steve Sideris, Adrian Folkes, Vickie Tsui, Irina Chuckowree, Daniel P. Sutherlin, Alan G. Olivero, David A. Peterson, Bing-Yan Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2408-2411
Efforts to identify potent small molecule inhibitors of PI3 kinase and mTOR led to the discovery of the exceptionally potent 6-aryl morpholino thienopyrimidine 6. In an effort to reduce the melting point in analogs of 6, the thienopyrimidine was modi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07054715432864ef6433675ccce8e7b4
https://doi.org/10.1016/j.bmcl.2010.03.046
https://doi.org/10.1016/j.bmcl.2010.03.046
Autor:
Shumei Wang, Susan Wong, Laurent Salphati, Simon Mathieu, John Lesnick, Deepak Sampath, Nan Chi Wan, Jodie Pang, Irina Chuckowree, Alan G. Olivero, Cristina Lewis, Daniel P. Sutherlin, Jim Nonomiya, Adrian Folkes, Zhigang Chang, Christian Wiesmann, Tim Heffron, Lori Friedman, Jenna Dotson, Richard Goldsmith, Georgette Castanedo, Wei Wei Prior, Steve Sideris, Leslie Lee, Vickie Tsui, Qingping Tian, Bing-Yan Zhu, Megan Berry
Publikováno v:
Journal of Medicinal Chemistry. 53:1086-1097
The PI3K/AKT/mTOR pathway has been shown to play an important role in cancer. Starting with compounds 1 and 2 (GDC-0941) as templates, (thienopyrimidin-2-yl)aminopyrimidines were discovered as potent inhibitors of PI3K or both PI3K and mTOR. Structur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a01dbe4957dc3c1f294e6e22c73dcc85
https://doi.org/10.1021/jm901284w
https://doi.org/10.1021/jm901284w
Autor:
Adrian Folkes, Alexis De Haven Brandon, Sonal Patel, Francesca Di Stefano, Letitia Lensun, Peter Sheldrake, Alexander Zhyvoloup, Irina Chuckowree, Stephen J. Shuttleworth, Suzanne A. Eccles, Melanie Valenti, Sonia Alix, Paul A. Clarke, Nahid Saghir, Nan Chi Wan, Paul Workman, Alan T. Henley, Edward McDonald, Gary Box, Anthony Robson, Giles Pergl-Wilson, Florence I. Raynaud, Angela Hayes, Sharon Gowan
Publikováno v:
Molecular Cancer Therapeutics. 8:1725-1738
The phosphatidylinositide 3-kinase pathway is frequently deregulated in human cancers and inhibitors offer considerable therapeutic potential. We previously described the promising tricyclic pyridofuropyrimidine lead and chemical tool compound PI-103
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d53d2116412a4ec9393dec9e50aa6961
https://doi.org/10.1158/1535-7163.mct-08-1200
https://doi.org/10.1158/1535-7163.mct-08-1200
Autor:
Suzanne A. Eccles, Pauline Moore, Lori Friedman, Paul A. Clarke, Stewart J. Baker, Olivero Alan G, Gary Box, Anthony Robson, Paul Workman, Khatereh Ahmadi, Laurent Salphati, Nahid Saghir, Giles Pergl-Wilson, Irina Chuckowree, Mark H. Ultsch, Wendy K. Alderton, Marketa Zvelebil, Florence I. Raynaud, Sukhjit Sohal, Arumugam Kugendradas, Christian Wiesmann, Adrian Folkes, Sonal Patel, Letitia Lensun, Angela Hayes, Timothy Hancox, Stephen J. Shuttleworth, Alexander Zhyvoloup, Heidi J.A. Wallweber, Paul Depledge, Melanie Valenti, Sonia Alix, Nan Chi Wan, Jodie Pang
Publikováno v:
Journal of Medicinal Chemistry. 51:5522-5532
Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9de0e3ae091925e99a0f90135c014d5f
https://doi.org/10.1021/jm800295d
https://doi.org/10.1021/jm800295d