- Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics**
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Protein arginine N-methyl transferase 4 (PRMT4) asymmetrically dimethylates the arginine residues of histone H3 and nonhistone proteins. The overexpression of PRMT4 in several cancers has stimulated interest in the discovery of inhibitors as biological tools and, potentially, therapeutics. Although several PRMT4 inhibitors have been reported, most display poor selectivity against other members of the PRMT family of methyl transferases. Herein, we report the structure-based design of a new class of alanine-containing 3-arylindoles as potent and selective PRMT4 inhibitors, and describe key structure–activity relationships for this class of compounds.
- Sutherland, Mathew,Li, Alice,Kaghad, Anissa,Panagopoulos, Dimitrios,Li, Fengling,Szewczyk, Magdalena,Smil, David,Scholten, Cora,Bouché, Léa,Stellfeld, Timo,Arrowsmith, Cheryl H.,Barsyte, Dalia,Vedadi, Masoud,Hartung, Ingo V.,Steuber, Holger,Britton, Robert,Santhakumar, Vijayaratnam
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supporting information
p. 1116 - 1125
(2021/03/08)
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- LXR MODULATORS
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The present invention provides compounds of Formula I and Formula II: or pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXRs), and compositions comprising any of such novel compounds and methods of use thereof. These compounds are useful as medicaments for treatment and/or prophylaxis for diseases or conditions related to activity of LXRs.
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Page/Page column 61
(2014/10/04)
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- LXR MODULATORS
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The present invention provides compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXR), compositions comprising any of such novel compounds, methods of using these compounds or compositions as medicaments for prevention or treatment of diseases or disorders related to liver X receptor (LXR), as well as methods of preparing these LXR modulators and using them in the manufacture of medicaments.
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Page/Page column 70
(2014/09/29)
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- A novel method for the conversion of carboxylic acids to N,N-dimethylamides using N,N-dimethylacetamide as a dimethylamine source
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A simple, cost effective and environmentally benign method is reported for the preparation of N,N-dimethylamides from carboxylic acids. The versatility of the method is determined by synthesising a large number of N,N-dimethylamide derivatives. Carboxylic acids are heated at 160-165°C in N,N-dimethylacetamide solvent in the presence of1,1'-carbonyldiimidazole to afford the corresponding N,N-dimethylamides in good to excellent yields.
- Aavula, Sanjeev Kumar,Chikkulapally, Anil,Hanumanthappa,Jyothi, Indira,Vinod,Sulur, Kumar,Manjunatha,Sythana, Suresh Kumar
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p. 155 - 159
(2013/07/11)
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- PHENOXY ACETIC ACID DERIVATIVES
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The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
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Page/Page column 136
(2010/09/03)
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- Transition Metal Phosphine Complexes Possessing Phase Transfer Function. Preparation and Reactivities of Palladium Complexes Containing Quaternary Ammonium Groups
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A new type of phosphine ligands (L) bearing quaternary ammonium as a functional group was synthesized.Their palladium complexes, PdBr2L2, readily underwent halogen exchange with powdered NaI under two-phase conditions, and efficiently catalyzed the fluorocarbonylation of phenyl bromide with powdered KF at atmospheric pressure of CO.
- Okano, Tamon,Harada, Nobuyuki,Kiji, Jitsuo
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p. 1057 - 1060
(2007/10/02)
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