7-MORPHOLINO-L,6-NAPHTHYRIDIN-5-YL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF USEFUL AS DNA-PK INHIBITOR

The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and...

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Hauptverfasser: HSIEH, Tom Han Hsiao, YEE, Leanna, PAQUETTE, Jay John, ARNS, Stephen Paul, OSBORNE, Simon, SMYTH, Elliott, KYLE, Alastair H, MINCHINTON, Andrew I, SHIDMOOSSAVEE, Fahimeh S, HAMBY, Callum, AMBLER, Martin, JAQUITH, James Brian, TAN, Jason Samuel, BAKER, Jennifer H. E, SMILJANIC-HURLEY, Ela
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creator HSIEH, Tom Han Hsiao
YEE, Leanna
PAQUETTE, Jay John
ARNS, Stephen Paul
OSBORNE, Simon
SMYTH, Elliott
KYLE, Alastair H
MINCHINTON, Andrew I
SHIDMOOSSAVEE, Fahimeh S
HAMBY, Callum
AMBLER, Martin
JAQUITH, James Brian
TAN, Jason Samuel
BAKER, Jennifer H. E
SMILJANIC-HURLEY, Ela
description The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula.
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subjects BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS THEREOF
CULTURE MEDIA
ENZYMOLOGY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SPIRITS
VINEGAR
WINE
title 7-MORPHOLINO-L,6-NAPHTHYRIDIN-5-YL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF USEFUL AS DNA-PK INHIBITOR
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