656226-63-0Relevant academic research and scientific papers
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors
Price, Steve,Bordogna, Walter,Bull, Richard J.,Clark, David E.,Crackett, Peter H.,Dyke, Hazel J.,Gill, Matthew,Harris, Neil V.,Gorski, Julia,Lloyd, Julia,Lockey, Peter M.,Mullett, Julia,Roach, Alan G.,Roussel, Fabien,White, Anne B.
, p. 370 - 375 (2007/10/03)
Optimisation of ADS100380, a sub-micromolar HDAC inhibitor identified using a virtual screening approach, led to a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids (6a-i), that possessed significant HDAC inhibitory activity. Subseque
SUBSTITUTED THIENYL-HYDROXAMIC ACIDS HAVING HISTONE DEACETYLASE ACTIVITY
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Page/Page column 54, (2010/02/10)
A compound of formula (I): in which A represents optionally substituted monocyclic heteroaryl or phenyl B represents optionally substituted heteroaryl, aryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl X and Y, which may be the same or different, each independently represent -0-, -NR1-, CO-, -S02-, -SO-, -S-, -NR1CO-, -NR1S02-, -CONR1-, -SO2NR1-, -NR1CONR1 or X may be a direct bond when Y represents -NR1-, -NR1CO-, -NR1SO2-, -CONR1-, - SO2NR1- or -NR1CONRI- provided that R1 represents alkyl substituted by -OR2,-NR3R4, - NR4COR5, -NR4SO2R5, -CONR3R4 or -S02NR3R4 R1 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, or alkyl substituted by -OR2, -NR3R4, -NR4COR5, -NR4S02R5, -CONR3R4 or -S02NR3R4 R2 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl R3 represents H or alkyl R4 represents H, alkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl or cycloalkyl or NR3R4 represents a cyclic amine R5 represents alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkylalkyl n represents 0-3 m represents 1-3 p represents 0-3 and corresponding N-oxides, pharmaceutically acceptable salts, solvates and prodrugs thereof; and use to treat a disease in which inhibition of histone deacetylase can prevent, inhibit or ameliorate the pathology and/or symptomatology of the disease.
SUBSTITUTED THIENYL-HYDROXAMIC ACIDS AS HISTONE DEACETYLASE INHIBITORS
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A compound of formula (I): which can be used in the treatment of diseases associated with histone deacetylase enzymatic activity.
