Search Results - "Barton, Naomi"
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Structure–activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling
Published in Scientific reports (11-02-2024)“…The tetrasubstituted naphthalene diimide compound QN-302 binds to G-quadruplex (G4) DNA structures. It shows high potency in pancreatic ductal adenocarcinoma…”
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Identification of the Clinical Candidate (R)‑(1-(4-Fluorophenyl)-6-((1-methyl‑1H‑pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro‑1H‑pyrazolo[3,4‑g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist
Published in Journal of medicinal chemistry (27-04-2017)“…The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing’s…”
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Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models
Published in ACS medicinal chemistry letters (13-08-2020)“…Targeting of genomic quadruplexes is an approach to treating complex human cancers. We describe a series of tetra-substituted naphthalene diimide (ND)…”
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Accessing low-oxidation state taxanes: is taxadiene-4(5)-epoxide on the taxol biosynthetic pathway?
Published in Chemical science (Cambridge) (01-01-2016)“…We have shown for the first time that taxadiene ( 3 ) can be epoxidised in a regio- and diastereoselective manner to provide taxadiene-4(5)-epoxide ( 12 ) as a…”
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Identification of the Clinical Candidate ( R )-(1-(4-Fluorophenyl)-6-((1-methyl-1 H -pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1 H -pyrazolo[3,4- g ]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist
Published in Journal of medicinal chemistry (27-04-2017)Get full text
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Accessing low-oxidation state taxanes: is taxadiene-4(5)-epoxide on the taxol biosynthetic pathway?† †Electronic supplementary information (ESI) available: Full experimental procedures and copies of 1H and 13C NMR spectra. CCDC 1030909. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c5sc03463a
Published in Chemical science (Cambridge) (26-01-2016)“…We report the first synthesis of taxadiene-4(5)-epoxide, which rearranges upon acid treatment to produce products of relevance to taxol biosynthesis. We have…”
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