Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Christian Bubert"'
Autor:
Oliver B. Sutcliffe, L. W. Lawrence Woo, Mary F. Mahon, Atul Purohit, Barry V. L. Potter, Christian Bubert, Surinder K. Chander, Michael J. Reed
Publikováno v:
ChemMedChem. 3:1708-1730
4-(((4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)phenyl sulfamate (6 a) was the first dual aromatase-sulfatase inhibitor (DASI) reported. Several series of its derivatives with various linker systems between the steroid sulfatase (STS) and the
Autor:
Shiuan A. Chen, Oliver B. Sutcliffe, Atul Purohit, Christian Bubert, Dujin J. Zhou, Barry V. L. Potter, Simon P. Newman, Surinder K. Chander, L. W. Lawrence Woo, Paul A. Foster, Michael J. Reed
Publikováno v:
Clinical Cancer Research. 14:6469-6477
Purpose: The production of E2 is paramount for the growth of estrogen receptor–positive breast cancer. Various strategies have been used, including the use of enzyme inhibitors against either aromatase (AROM) or steroid sulfatase (STS), in an attem
Autor:
Helena J. Tutill, Nigel Vicker, Mary F. Mahon, Barry V. L. Potter, Joanna M. Day, Gillian M. Allan, Atul Purohit, Christian Bubert, Michael J. Reed, Harshani R. Lawrence, Andrew Smith
Publikováno v:
ChemMedChem. 1:464-481
17 beta-Hydroxysteroid dehydrogenase type 1 (17 beta-HSD1), an oxidoreductase which has a preferential reductive activity using NADPH as cofactor, converts estrone to estradiol and is expressed in many steroidogenic tissues including breast and in ma
Autor:
Helena J. Tutill, Christian Bubert, Mary F. Mahon, Josephine Cornet, Gillian M. Allan, Nigel Vicker, Andrew Smith, Joanna M. Day, Michael J. Reed, Barry V. L. Potter, Atul Purohit, Delphine S. Fischer, Harshani Rithma Ruchiranani Lawrence
Publikováno v:
Journal of Medicinal Chemistry. 49:1325-1345
The 17beta-hydroxysteroid dehydrogenases (17beta-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17beta-HSD type 1 enzyme (17beta-HSD1) catalyzes the reduction of estrone to
Autor:
Annette G. Beck-Sickinger, Raphael Beumer, Oliver Reiser, Norman Koglin, Chiara Zorn, Chiara Cabrele, Christian Bubert, Norbert Sewald
Publikováno v:
Angewandte Chemie. 115:212-215
Binding mode and structure-activity relationships around direct inhibitors of the Nrf2-Keap1 complex
Autor:
Edward Beaumont, Mark A. Brooks, Eric Jnoff, Vincent Anthony Corden, Christophe Genicot, Stephanie Duclos, John J. Barker, Zara A. Sands, Graham Dawson, Oliver Barker, Steven Bromidge, Rosemary Maghames, Claudia Albrecht, Jason Kwong, Jean-Philippe Courade, Tara Fryatt, Richard Pike, Tom Ceska, Frederick Arthur Brookfield, Emilie Jigorel, Innocent Mushi, Christian Bubert, Christopher C. Stimson, Myron A. Smith
Publikováno v:
ChemMedChem. 9(4)
An X-ray crystal structure of Kelch-like ECH-associated protein(Keap1) co-crystallised with (1S,2R)-2-[(1S)-1-[(1,3-dioxo-2,3-di-hydro-1H-isoindol-2-yl)methyl]-1,2,3,4-tetrahydroisoquinolin-2-carbonyl]cyclohexane-1-carboxylic acid (compound (S,R,S)-1
Autor:
Emilio Parisini, Oliver Reiser, Thomas Labahn, Marina Schinnerl, Claudius Böhm, Manfred Zabel, Christian Bubert
Publikováno v:
Scopus-Elsevier
The stereoselective synthesis of highly functionalized 1,2,3-trisubstituted cyclopropanes 1 and 2, starting from readily available furans 3 or N-protected pyrrole 4, is described. Furthermore, exceptionally high diastereocontrol in agreement with the
Autor:
Christian Bubert, Oliver Reiser
Publikováno v:
Tetrahedron Letters. 38:4985-4988
Exceptionally high diastereocontrol in agreement with the Felkin-Anh model was observed for the addition of nucleophiles to the β-aminocyclopropylcarbaldehyde 5 in nitroaldol, cyanohydrin, Mukaiyama aldol, and Sakurai reactions, contrasting the low
Autor:
L W Lawrence, Woo, Paul M, Wood, Christian, Bubert, Mark P, Thomas, Atul, Purohit, Barry V L, Potter
Publikováno v:
Chemmedchem
4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs). Structure–activity relationship studies were performed o
Autor:
Steven Fitzjohn, John Crosby, Christian Bubert, Stephen M. Brown, John Blacker, Tim Thorpe, Jonathan M. J. Williams, James Peter Muxworthy
Publikováno v:
Tetrahedron Letters. 42:4037-4039
Water-soluble analogues of Noyori's (1S,2S)-N-(p-tolylsulfonyl)-1,2-diphenylethylenediamine and Knochel's (1R,2R)-N-(p-tolylsulfonyl)-1,2-diaminocyclohexane, containing an additional sulfonic acid group, have been synthesised. The ruthenium catalysed