- INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
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The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
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Page/Page column 57; 71-72
(2020/10/20)
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- Synthesis of β-Amino Diaryldienones Using the Mannich Reaction
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The Mannich reaction has been used for decades to prepare many pharmaceutically important molecules. Here, using a "double-Mannich-β-elimination" synthetic sequence, we report the synthesis and the characterization details of a novel class of β-amino diaryldienones with prominent antiprostate cancer activity. Through these studies, we correct an erroneous structure in the current literature, present a discussion of the stereochemical outcome of a new reaction, and probe the mechanism(s) of byproduct formation through isotopic studies.
- Elshan, N. G. R. Dayan,Rettig, Matthew B.,Jung, Michael E.
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supporting information
(2019/06/13)
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- INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
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The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
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- An investigation of the scope of the 1,7-electrocyclization of α,β:γ,δ-conjugated azomethine ylides
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Substituents on the diene component have little influence on the periselectivity of the cyclizations of α,β:γ,δ-conjugated azomethine ylides, with 1,7-electrocyclizations predominating. In some cases, subtle changes to these substituents can, however, influence the product formed, through their effect on the relative energies of the transition states for the 1,5- (6π) and 1,7-electrocyclization (8π) processes. The most striking changes in periselectivity occur for phenylethenyl-substituted azomethine ylides 3d-f, which can give either a pyrroline 4d,f or dihydrobenzazepine 6e, depending upon the alkene configuration.
- Zhang, Weimin,Ning, Fuqiang,Váradi, Linda,Hibbs, David E.,Platts, James A.,Nyerges, Miklós,Anderson, Rosaleen J.,Groundwater, Paul W.
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supporting information
p. 3621 - 3629
(2014/05/20)
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- Ruthenium-catalyzed aldehyde functionality reshuffle: Selective synthesis of E-2-arylcinnamaldehydes from E-β-bromostyrenes and aryl aldehydes
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A new concept for highly selective synthesis of E-2-arylcinnamaldehydes has been developed via a formal arylformylation of E-β-bromostyrenes with readily available aryl aldehydes. This strategy involves an overall reshuffle of the aldehyde functionality with a loss of hydrogen bromide.
- Wang, Ping,Rao, Honghua,Zhou, Feng,Li, Chao-Jun,Hua, Ruimao
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supporting information
p. 16468 - 16471,4
(2020/09/15)
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