-
1
-
-
85012009358
-
Estrogen receptors as therapeutic targets in breast cancer
-
In. Eckhard, O. Weinmann, H. Wiley-VCH Verlag GmbH: Weinheim, Germany
-
Ariazi, E. A.; Jordan, V. C. Estrogen receptors as therapeutic targets in breast cancer. In Nuclear Receptors as Drug Targets. Eckhard, O., Weinmann, H., Eds.; Wiley-VCH Verlag GmbH: Weinheim, Germany, 2008; pp 127-199.
-
(2008)
Nuclear Receptors As Drug Targets
, pp. 127-199
-
-
Ariazi, E.A.1
Jordan, V.C.2
-
2
-
-
0037364074
-
Tamoxifen: A most unlikely pioneering medicine
-
Jordan, V. C. Tamoxifen: a most unlikely pioneering medicine Nat. Rev. Drug Discovery 2003, 2, 205-213 10.1038/nrd1031
-
(2003)
Nat. Rev. Drug Discovery
, vol.2
, pp. 205-213
-
-
Jordan, V.C.1
-
3
-
-
0032581614
-
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene
-
Rosati, R. L.; Jardine, P. D. S.; Cameron, K. O.; Thompson, D. D.; Ke, H. Z.; Toler, S. M.; Brown, T. A.; Pan, L. C.; Ebbinghaus, C. F.; Reinhold, A. R.; Elliott, N. C.; Newhouse, B. N.; Tjoa, C. M.; Sweetnam, P. M.; Cole, M. J.; Arriola, M. W.; Gauthier, J. W.; Crawford, D. T.; Nickerson, D. F.; Pirie, C. M.; Qi, H.; Simmons, H. A.; Tkalcevic, G. T. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene J. Med. Chem. 1998, 41, 2928-2931 10.1021/jm980048b
-
(1998)
J. Med. Chem.
, vol.41
, pp. 2928-2931
-
-
Rosati, R.L.1
Jardine, P.D.S.2
Cameron, K.O.3
Thompson, D.D.4
Ke, H.Z.5
Toler, S.M.6
Brown, T.A.7
Pan, L.C.8
Ebbinghaus, C.F.9
Reinhold, A.R.10
Elliott, N.C.11
Newhouse, B.N.12
Tjoa, C.M.13
Sweetnam, P.M.14
Cole, M.J.15
Arriola, M.W.16
Gauthier, J.W.17
Crawford, D.T.18
Nickerson, D.F.19
Pirie, C.M.20
Qi, H.21
Simmons, H.A.22
Tkalcevic, G.T.23
more..
-
4
-
-
77950634822
-
Fulvestrant - A novel endocrine therapy for breast cancer
-
Johnston, S. J.; Cheung, K. L. Fulvestrant-a novel endocrine therapy for breast cancer Curr. Med. Chem. 2010, 17, 902-914 10.2174/092986710790820633
-
(2010)
Curr. Med. Chem.
, vol.17
, pp. 902-914
-
-
Johnston, S.J.1
Cheung, K.L.2
-
5
-
-
84928485170
-
Investigation of (E)-3-[4-(2-oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic acids as Oral Selective Estrogen Receptor Down-Regulators
-
Degorce, S. L.; Bailey, A.; Callis, R.; De Savi, C.; Ducray, R.; Lamont, G.; MacFaul, P. A.; Maudet, M.; Martin, S.; Morgentin, R.; Norman, R. A.; Peru, A.; Pink, J.; Plé, P.; Roberts, B.; Scott, J. S. Investigation of (E)-3-[4-(2-oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic acids as Oral Selective Estrogen Receptor Down-Regulators J. Med. Chem. 2015, 58 (8) 3522-3533 10.1021/acs.jmedchem.5b00066
-
(2015)
J. Med. Chem.
, vol.58
, Issue.8
, pp. 3522-3533
-
-
Degorce, S.L.1
Bailey, A.2
Callis, R.3
De Savi, C.4
Ducray, R.5
Lamont, G.6
MacFaul, P.A.7
Maudet, M.8
Martin, S.9
Morgentin, R.10
Norman, R.A.11
Peru, A.12
Pink, J.13
Plé, P.14
Roberts, B.15
Scott, J.S.16
-
6
-
-
84933059419
-
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts
-
Lai, A.; Kahraman, M.; Govek, S.; Nagasawa, J.; Bonnefous, C.; Julien, J.; Douglas, K.; Sensintaffar, J.; Lu, N.; Lee, K.-j.; Aparicio, A.; Kaufman, J.; Qian, J.; Shao, G.; Prudente, R.; Moon, M. J.; Joseph, J. D.; Darimont, B.; Brigham, D.; Grillot, K.; Heyman, R.; Rix, P. J.; Hager, J. H.; Smith, N. D. Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts J. Med. Chem. 2015, 58 (12) 4888-4904 10.1021/acs.jmedchem.5b00054
-
(2015)
J. Med. Chem.
, vol.58
, Issue.12
, pp. 4888-4904
-
-
Lai, A.1
Kahraman, M.2
Govek, S.3
Nagasawa, J.4
Bonnefous, C.5
Julien, J.6
Douglas, K.7
Sensintaffar, J.8
Lu, N.9
Lee, K.-J.10
Aparicio, A.11
Kaufman, J.12
Qian, J.13
Shao, G.14
Prudente, R.15
Moon, M.J.16
Joseph, J.D.17
Darimont, B.18
Brigham, D.19
Grillot, K.20
Heyman, R.21
Rix, P.J.22
Hager, J.H.23
Smith, N.D.24
more..
-
7
-
-
84945381593
-
Optimization of a novel binding motif to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist
-
De Savi, C.; Bradbury, R. H.; Rabow, A. A.; Norman, R. A.; de Almeida, C.; Andrews, D. M.; Ballard, P.; Buttar, D.; Callis, R. J.; Currie, G. S.; Curwen, J. O.; Davies, C. D.; Donald, C. S.; Feron, L. J. L.; Gingell, H.; Glossop, S. C.; Hayter, B. R.; Hussain, S.; Karoutchi, G.; Lamont, S. G.; MacFaul, P.; Moss, T. A.; Pearson, S. E.; Tonge, M.; Walker, G. E.; Weir, H. M.; Wilson, Z. Optimization of a novel binding motif to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist J. Med. Chem. 2015, 58 (20) 8128-8140 10.1021/acs.jmedchem.5b00984
-
(2015)
J. Med. Chem.
, vol.58
, Issue.20
, pp. 8128-8140
-
-
De Savi, C.1
Bradbury, R.H.2
Rabow, A.A.3
Norman, R.A.4
De Almeida, C.5
Andrews, D.M.6
Ballard, P.7
Buttar, D.8
Callis, R.J.9
Currie, G.S.10
Curwen, J.O.11
Davies, C.D.12
Donald, C.S.13
Feron, L.J.L.14
Gingell, H.15
Glossop, S.C.16
Hayter, B.R.17
Hussain, S.18
Karoutchi, G.19
Lamont, S.G.20
MacFaul, P.21
Moss, T.A.22
Pearson, S.E.23
Tonge, M.24
Walker, G.E.25
Weir, H.M.26
Wilson, Z.27
more..
-
8
-
-
2342614324
-
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists
-
Chesworth, R.; Zawistoski, M. P.; Lefker, B. A.; Cameron, K. O.; Day, R. F.; Mangano, F. M.; Rosati, R. L.; Colella, S.; Petersen, D. N.; Brault, A.; Lu, B.; Pan, L. C.; Perry, P.; Ng, O.; Castleberry, T. A.; Owen, T. A.; Brown, T. A.; Thompson, D. D.; DaSilva-Jardine, Paul Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists Bioorg. Med. Chem. Lett. 2004, 14 (11) 2729-2733 10.1016/j.bmcl.2004.03.077
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, Issue.11
, pp. 2729-2733
-
-
Chesworth, R.1
Zawistoski, M.P.2
Lefker, B.A.3
Cameron, K.O.4
Day, R.F.5
Mangano, F.M.6
Rosati, R.L.7
Colella, S.8
Petersen, D.N.9
Brault, A.10
Lu, B.11
Pan, L.C.12
Perry, P.13
Ng, O.14
Castleberry, T.A.15
Owen, T.A.16
Brown, T.A.17
Thompson, D.D.18
DaSilva-Jardine, P.19
-
9
-
-
0038798608
-
Estrogen Receptor Modulators: Identification and Structure-Activity Relationships of Potent ERα-Selective Tetrahydroisoquinoline Ligands
-
Renaud, J.; Bischoff, S. F.; Buhl, T.; Floersheim, P.; Fournier, B.; Halleux, C.; Kallen, J.; Keller, H.; Schlaeppi, J.-M.; Stark, W. Estrogen Receptor Modulators: Identification and Structure-Activity Relationships of Potent ERα-Selective Tetrahydroisoquinoline Ligands J. Med. Chem. 2003, 46 (14) 2945-2957 10.1021/jm030086h
-
(2003)
J. Med. Chem.
, vol.46
, Issue.14
, pp. 2945-2957
-
-
Renaud, J.1
Bischoff, S.F.2
Buhl, T.3
Floersheim, P.4
Fournier, B.5
Halleux, C.6
Kallen, J.7
Keller, H.8
Schlaeppi, J.-M.9
Stark, W.10
-
10
-
-
19944431090
-
Selective Estrogen Receptor Modulators with Conformationally Restricted Side Chains. Synthesis and Structure-Activity Relationship of ERα-Selective Tetrahydroisoquinoline Ligands
-
Renaud, J.; Bischoff, S. F.; Buhl, T.; Floersheim, P.; Fournier, B.; Geiser, M.; Halleux, C.; Kallen, J.; Keller, H.; Ramage, P. Selective Estrogen Receptor Modulators with Conformationally Restricted Side Chains. Synthesis and Structure-Activity Relationship of ERα-Selective Tetrahydroisoquinoline Ligands J. Med. Chem. 2005, 48 (2) 364-379 10.1021/jm040858p
-
(2005)
J. Med. Chem.
, vol.48
, Issue.2
, pp. 364-379
-
-
Renaud, J.1
Bischoff, S.F.2
Buhl, T.3
Floersheim, P.4
Fournier, B.5
Geiser, M.6
Halleux, C.7
Kallen, J.8
Keller, H.9
Ramage, P.10
-
11
-
-
84931301519
-
A Screening Assay Cascade to Identify and Characterize Novel Selective Estrogen Receptor Downregulators (SERDs)
-
Callis, R.; Rabow, A.; Tonge, M.; Bradbury, R.; Challinor, M.; Roberts, K.; Jones, K.; Walker, G. A Screening Assay Cascade to Identify and Characterize Novel Selective Estrogen Receptor Downregulators (SERDs) J. Biomol. Screening 2015, 20 (6) 748-759 10.1177/1087057115580298
-
(2015)
J. Biomol. Screening
, vol.20
, Issue.6
, pp. 748-759
-
-
Callis, R.1
Rabow, A.2
Tonge, M.3
Bradbury, R.4
Challinor, M.5
Roberts, K.6
Jones, K.7
Walker, G.8
-
12
-
-
84902524040
-
Reactive Metabolite Trapping Screens and Potential Pitfalls: Bioactivation of a Homomorpholine and Formation of an Unstable Thiazolidine Adduct
-
GSH trapping was assessed in human liver microsomes with trapping reported as a ratio to a positive control, clozapine, as detailed in
-
GSH trapping was assessed in human liver microsomes with trapping reported as a ratio to a positive control, clozapine, as detailed in Lenz, E. M.; Martin, S.; Schmidt, R.; Morin, P.-E.; Smith, R.; Weston, D. J.; Bayrakdarian, M. Reactive Metabolite Trapping Screens and Potential Pitfalls: Bioactivation of a Homomorpholine and Formation of an Unstable Thiazolidine Adduct Chem. Res. Toxicol. 2014, 27, 968-980 10.1021/tx5000409
-
(2014)
Chem. Res. Toxicol.
, vol.27
, pp. 968-980
-
-
Lenz, E.M.1
Martin, S.2
Schmidt, R.3
Morin, P.-E.4
Smith, R.5
Weston, D.J.6
Bayrakdarian, M.7
-
13
-
-
33748129547
-
Optimisation and validation of a medium-throughput electrophysiology-based hERG assay using IonWorks HT
-
Bridgland-Taylor, M. H.; Hargreaves, A. C.; Easter, A.; Orme, A.; Henthorn, D. C.; Ding, M.; Davis, A. M.; Small, B. G.; Heapy, C. G.; Abi-Gerges, N.; Persson, F.; Jacobson, I.; Sullivan, M.; Albertson, N.; Hammond, T. G.; Sullivan, E.; Valentin, J.-P.; Pollard, C. E. Optimisation and validation of a medium-throughput electrophysiology-based hERG assay using IonWorks HT J. Pharmacol. Toxicol. Methods 2006, 54, 189-199 10.1016/j.vascn.2006.02.003
-
(2006)
J. Pharmacol. Toxicol. Methods
, vol.54
, pp. 189-199
-
-
Bridgland-Taylor, M.H.1
Hargreaves, A.C.2
Easter, A.3
Orme, A.4
Henthorn, D.C.5
Ding, M.6
Davis, A.M.7
Small, B.G.8
Heapy, C.G.9
Abi-Gerges, N.10
Persson, F.11
Jacobson, I.12
Sullivan, M.13
Albertson, N.14
Hammond, T.G.15
Sullivan, E.16
Valentin, J.-P.17
Pollard, C.E.18
|