85064-61-5Relevant articles and documents
Synthesis and activity of putative small-molecule inhibitors of the F-box protein SKP2
Shouksmith, Andrew E.,Evans, Laura E.,Tweddle, Deborah A.,Miller, Duncan C.,Willmore, Elaine,Newell, David R.,Golding, Bernard T.,Griffin, Roger J.
, p. 660 - 679 (2015/04/27)
The tetrahydropyran 4-(((3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-4-phenylbutyl)amino)methyl)-N,N-dimethylaniline was reported to disrupt the SCFSKP2 E3 ligase complex. Efficient syntheses of this tetrahydropyran derivative and analogues, including the des-dimethyl derivative 4-(((3-(tetrahydro-2H-pyran-4-yl)-4-phenylbutyl)amino)methyl)-N,N-dimethylaniline, are described. The enantiomers of the des-dimethyl compound were obtained using Evans' chiral auxiliaries. Structure-activity relationships for these tetrahydropyrans and analogues have been determined by measurement of growth-inhibitory activities in HeLa cells, which indicated a non-specific mechanism of action that correlates with inhibitor lipophilicity. However, preliminary data with (R)-and (S)-4-(((3-(tetrahydro-2H-pyran-4-yl)-4-phenylbutyl)amino)methyl)-N,N-dimethylaniline showed enantioselective inhibition of the degradation of p27 in a cell-based assay that acts as a reporter of SKP2 activity.
COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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, (2015/02/02)
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
Hepatitis C Virus Inhibitors
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, (2015/02/25)
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
NDM INHIBITOR
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, (2014/06/24)
An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):
HYDROXAMATE SULFONAMIDES AS CD23 SHEDDING INHIBITORS
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Page 30, (2010/02/10)
A class of piperidine and related heterocyclic derivatives, C-substituted by a substituted aryl or heteroaryl moiety, and N-substituted by an ethylsulfonyl group which in turn is substituted at the 2-position by a hydroxamic acid moiety and also by a range of alternative substituents, being potent inhibitors of CD23 shedding, are useful in the treatment and/or prevention of allergic, inflammatory and neoplastic diseases.
HYDROXAMATE SULFONAMIDES AS CD23 SHEDDING INHIBITORS
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Page 23, (2010/02/10)
A class of piperazine and related heterocyclic derivatives, substituted at the 4-position by a substituted aryl or heteroaryl moiety, and at the 1-position by an ethylsulfonyl group which in turn is substituted at the 2-position by a hydroxamic acid moiety and also by a range of alternative substituents, being potent inhibitors of CD23 shedding, are useful in the treatment and/or prevention of allergic, inflammatory and neoplastic diseases.
BENZO(5,6)CYCLOHEPTA(1,2-B)PYRIDINE DERIVATIVES USEFUL FOR INHIBITION OF FARNESYL PROTEIN TRANSFERASE
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Page 51, (2010/02/08)
Novel compounds of formula (1.0) are disclosed. In Formula (1.0) a represents N or NO, R and R are halo, R and R are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
Compounds useful for inhibition of farnesyl protein transferase
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, (2008/06/13)
Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1and R3are halo, R2and R4are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
Potent HIV Protease Inhibitors: The Development of Tetrahydrofuranylglycines as Novel P2 Ligands and Pyrazine Amides as P3-Ligands
Ghosh, Arun K.,Thompson, Wayne J.,Holloway, M. Katharine,McKee, Sean P.,Duong, Tien T.,et al.
, p. 2300 - 2310 (2007/10/02)
A series of protease inhibitors bearing constrained unnaturel amino acids at the P2-position and novel heterocycles at the P3-position of compound 1 (Ro 31-8959) were synthesized, and their in vitro enzyme inhibitory and antiviral ac
TRIAZOLO-1,4-DIAZEPINE DERIVATIVES AND THEIR USE IN PHARMACEUTICALS
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, (2008/06/13)
A triazolo-1,4-di-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. STR1 in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is--OCO--,--NHCO--,--CO--or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.