Patent classifications
C07C50/30
IRON CATALYZED HIGHLY ENANTIOSELECTIVE CIS-DIHYDROXYLATION OF QUINONES
Methods for asymmetric cis-dihydroxylation (“AD”) of quinones to produce cis-diols of quinones with high yield (i.e. a yield ≥30%) and high enantioselectivity (i.e. an enantiometric excess ≥30%) are disclosed. The method uses an iron-based catalyst, such as one or more Fe(II) complexes, as the catalyst, and can be performed under mild reaction conditions (e.g. a temperature ≤50° C. at 1 atom in open air). The method generally includes: (i) maintaining a reaction mixture at a temperature for a period of time sufficient to form a product, where the reaction mixture contains a quinone, one or more iron-based catalyst(s), and a solvent, and where the product contains a chiral cis-diol. Optionally, the method also includes adding an oxidant into the reaction mixture prior to and/or during step (i), such as a hydrogen peroxide solution.
IRON CATALYZED HIGHLY ENANTIOSELECTIVE CIS-DIHYDROXYLATION OF QUINONES
Methods for asymmetric cis-dihydroxylation (“AD”) of quinones to produce cis-diols of quinones with high yield (i.e. a yield ≥30%) and high enantioselectivity (i.e. an enantiometric excess ≥30%) are disclosed. The method uses an iron-based catalyst, such as one or more Fe(II) complexes, as the catalyst, and can be performed under mild reaction conditions (e.g. a temperature ≤50° C. at 1 atom in open air). The method generally includes: (i) maintaining a reaction mixture at a temperature for a period of time sufficient to form a product, where the reaction mixture contains a quinone, one or more iron-based catalyst(s), and a solvent, and where the product contains a chiral cis-diol. Optionally, the method also includes adding an oxidant into the reaction mixture prior to and/or during step (i), such as a hydrogen peroxide solution.
Inhibition of DYRK1A kinase
Novel compounds which inhibit DYRK1A activity comprise thymoquinone derivatives including a pair of substituted or unsubstituted six-membered carbon rings selected from phenyl and cyclohexadiene linked by an alkyl or alkenyl linker. Each six-membered ring includes at least one oxygen-bearing substituent selected from carbonyl oxygens, hydroxyls, alkoxyls, and halogenated derivatives thereof. The compounds can be administered to mammalian subjects for inhibition of DYRK1A kinase proteins.
ANTI-BACTERIAL STILBENE DERIVATIVES AND METHODS OF USE
Provided herein are novel antibacterial compounds of Formula I. The compounds can be made through enzymatic oxidative dimerization in the presence of a suitable organism and one or more metal salts. Pathogenic bacteria exposed to the compound of Formula I do not develop resistance to these compounds even after prolonged exposure. Also provided herein are methods of treating bacterial infections, and method of killing or disinfecting bacteria.
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INHIBITION OF DYRK1A KINASE
Novel compounds which inhibit DYRK1A activity comprise thymoquinone derivatives including a pair of substituted or unsubstituted six-membered carbon rings selected from phenyl and cyclohexadiene linked by an alkyl or alkenyl linker. Each six-membered ring includes at least one oxygen-bearing substituent selected from carbonyl oxygens, hydroxyls, alkoxyls, and halogenated derivatives thereof. The compounds can be administered to mammalian subjects for inhibition of DYRK1A kinase proteins.
Quinochalcone compound and uses thereof for treating cancer or inflammation
Presented herein is a quinochalcone compound that displays strong anti-cancer properties and provides for synergistic anti-cancer activity when used in combination with interferon β (IFN-β) or interferon γ (IFN-γ). Accordingly, compositions comprising a quinochalcone compound, or a quinochalcone compound and an interferon are disclosed herein for use in treating cancer. Also presented herein, in some embodiments, are methods of using a quinochalcone compound, and compositions thereof, to treat inflammation.
Quinochalcone compound and uses thereof for treating cancer or inflammation
Presented herein is a quinochalcone compound that displays strong anti-cancer properties and provides for synergistic anti-cancer activity when used in combination with interferon β (IFN-β) or interferon γ (IFN-γ). Accordingly, compositions comprising a quinochalcone compound, or a quinochalcone compound and an interferon are disclosed herein for use in treating cancer. Also presented herein, in some embodiments, are methods of using a quinochalcone compound, and compositions thereof, to treat inflammation.
NOVEL QUINOCHALCONE COMPOUND AND USES THEREOF FOR TREATING CANCER OR INFLAMMATION
Presented herein is a quinochalcone compound that displays strong anti-cancer properties and provides for synergistic anti-cancer activity when used in combination with interferon (IFN-) or interferon (IFN-). Accordingly, compositions comprising a quinochalcone compound, or a quinochalcone compound and an interferon are disclosed herein for use in treating cancer. Also presented herein, in some embodiments, are methods of using a quinochalcone compound, and compositions thereof, to treat inflammation.
NOVEL QUINOCHALCONE COMPOUND AND USES THEREOF FOR TREATING CANCER OR INFLAMMATION
Presented herein is a quinochalcone compound that displays strong anti-cancer properties and provides for synergistic anti-cancer activity when used in combination with interferon (IFN-) or interferon (IFN-). Accordingly, compositions comprising a quinochalcone compound, or a quinochalcone compound and an interferon are disclosed herein for use in treating cancer. Also presented herein, in some embodiments, are methods of using a quinochalcone compound, and compositions thereof, to treat inflammation.
Iron catalyzed highly enantioselective cis-dihydroxylation of quinones
Methods for asymmetric cis-dihydroxylation (AD) of quinones to produce cis-diols of quinones with high yield (i.e. a yield 30%) and high enantioselectivity (i.e. an enantiometric excess 30%) are disclosed. The method uses an iron-based catalyst, such as one or more Fe(II) complexes, as the catalyst, and can be performed under mild reaction conditions (e.g. a temperature 50 C. at 1 atom in open air). The method generally includes: (i) maintaining a reaction mixture at a temperature for a period of time sufficient to form a product, where the reaction mixture contains a quinone, one or more iron-based catalyst(s), and a solvent, and where the product contains a chiral cis-diol. Optionally, the method also includes adding an oxidant into the reaction mixture prior to and/or during step (i), such as a hydrogen peroxide solution.