- NSD FAMILY INHIBITORS AND METHODS OF TREATMENT THEREWITH
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Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.
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Paragraph 0423; 0425; 0438; 0457
(2019/07/03)
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- Synthesis and reactivity of dimethoxy-functionalised Troeger's base analogues
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Troeger's base analogues were prepared bearing methoxy groups in the 1,7-, 2,8-, 3,9- or 4,10-positions. These compounds were converted to their dihydroxy analogues in excellent yields upon treatment with boron tribromide and the 4,10-dihydroxy analogue could be prepared by directly from 4-hydroxyaniline. The synthetic utility of the dihydroxy-functionalised compounds as building blocks was demonstrated by the synthesis of a dialkoxy and a diester Troeger's base analogue.
- Malik, Qasim M.,Ijaz, Sadia,Craig, Donald C.,Try, Andrew C.
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experimental part
p. 5798 - 5805
(2011/08/21)
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- Effect of structural factors and solvent nature in bromination of anilines
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Reaction of electrophilic bromination of aniline containing various ortho, meta, and para substituents in the aromatic ring was studied. The optimal conditions for synthesis of mono-, di-, tri-, and tetrabromo derivatives of aniline and brominated analog of Aniline Black were found.
- Bagmanov
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p. 1570 - 1576
(2011/06/20)
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- Polymer-supported organotin reagents for regioselective halogenation of aromatic amines
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(Chemical Equation Presented) Polymer-supported triorganotin halides were used in the halogenation reaction of aromatic amines. Treatment of aromatic amines with n-butyllithium and polymer-supported organotin halides gave the corresponding polymer-bound N-triorganostannylamines, which by treatment with bromine or iodine monochloride gave the para-halogenated aromatic amines with high yields and high selectivities. The polymer-supported organotin halides reagents regenerated during the course of the halogenation reaction can be reused without loss of efficiency. The presence of tin residues in halogenated aromatic amines was also investigated and evaluated at under 20 ppm after three runs.
- Chretien, Jean-Mathieu,Zammattio, Francoise,Le Grognec, Erwan,Paris, Michael,Cahingt, Blanche,Montavon, Gilles,Quintard, Jean-Paul
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p. 2870 - 2873
(2007/10/03)
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- Heteroaryl substituted benzothiazole dioxetanes
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Chemiluminescent heteroaryl substituted benzothiazole 1,2-dioxetane compounds capable of producing light energy when decomposed are provided. These chemiluminescent compounds are represented by the general formula: The heteroaryl substituent Y can be, for
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- Synthesis of 2,6-disubstituted and 2,3,6-trisubstituted anilines
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A number of 2,6-disubstituted and 2,3,6-trisubstituted anilines have been prepared via the selective para dehalogenation of the corresponding anilines. Modification of the substituents on the amino nitrogen demonstrates that the selectivity is derived from steric rather than electronic effects. The effects of the choice of formate hydrogen donor, Pd catalyst, solvent, and temperature upon the efficiency and selectivity of the dehalogenation are discussed.
- Pews,Hunter,Wehrmeyer
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p. 4809 - 4820
(2007/10/02)
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- Halogenation Using Quaternary Ammonium Polyhalides. VI. Bromination of Aromatic Amines by Use of Benzyltrimethylammonium Tribromide
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The reaction of aromatic amines with benzyltrimethylammonium tribromide in dichloromethane-methanol containing calcium carbonate powder for 0.5 h at room temperature gave bromo-substituted aromatic amines in good yields.
- Kajigaeshi, Shoji,Kakinami, Takaaki,Inoue, Kazuhisa,Kondo, Manabu,Nakamura, Hiroko,et al.
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p. 597 - 599
(2007/10/02)
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