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US 8,557,823 B2Granted
Family of PFKFB3 inhibitors with anti-neoplastic activities
AssigneesAdvanced Cancer Therapeutics, LLC, University of Louisville Research Foundation, Inc.
InventorsGilles Tapolsky, Pooran Chand, John O. Trent, Sucheta Telang, Brian F. Clem, Jason A. Chesney
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Abstract
A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.
Claims3
A compound or an optical isomer or stereoisomer or racemic mixture thereof, the compound having the Formula:
- wherein Ar1 is substituted or unsubstituted and is selected from the group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 3,5-pyrimidinyl, and 2,4-pyrimidinyl, wherein Ar1 substitutions are selected from the group consisting of H, F, Cl, OH, alkyl, O-alkyl, amino, alkylamino, carboxyl, aminocarbonyl, alkylaminocarbonyl, and combinations thereof;
- Y6, Y11 and Y12, are independently selected from the group consisting of N and CR, wherein when one of Y6, Y11, or Y12 is N, the other two are CR;
- Y17, Y18, and Y19 are independently selected from the group consisting of N and CR, wherein when one of Y17, Y18, or Y19 is N, the other two are CR;
- each of Y7, Y8, Y9, Y10, Y13, Y14, Y15, and Y16 is CR;
- and
- each R is independently selected from the group consisting of H, F, OH, alkyl, amino, alkylamino, carboxyl, aminocarbonyl, alkylaminocarbonyl, and combinations thereof.
3 more elements
A compound selected from the group consisting of:
- 1-Naphthalen-2-yl-3-quinolin-2-yl-propenone;
- 1-Naphthalen-2-yl-3-quinolin-3-yl-propenone;
- 3-(4-Hydroxy-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 3-(8-Hydroxy-quinolin-2-yl)-1-pyridin-3-yl-propenone;
- 3-Quinolin-2-yl-1-p-tolyl-propenone;
- 3-(8-Hydroxy-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 3-(8-Hydroxy-quinolin-2-yl)-1-p-tolyl-propenone;
- 3-(4-Hydroxy-quinolin-2-yl)-1-p-tolyl-propenone;
- 1-Phenyl-3-quinolin-2-yl-propenone;
- 1-(2-Hydroxy-phenyl)-3-quinolin-2-yl-propenone;
- 1-(4-Hydroxy-phenyl)-3-quinolin-2-yl-propenone;
- 1-(2-Amino-phenyl)-3-quinolin-2-yl-propenone;
- 1-(4-Amino-phenyl)-3-quinolin-2-yl-propenone;
- 4-(3-Quinolin-2-yl-acryloyl)-benzamide;
- 4-(3-Quinolin-2-yl-acryloyl)-benzoic acid;
- 3-(8-Methyl-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 1-(2-Fluoro-pyridin-4-yl)-3-quinolin-2-yl-propenone;
- 3-(8-Fluoro-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 3-(6-Hydroxy-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 3-(8-Methylamino-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- 3-(7-Methyl-quinolin-2-yl)-1-pyridin-4-yl-propenone;
- and
- 1-Methyl-4-[3-(8-methyl-quinolin-2-yl)-acryloyl]-pyridinium.
20 more elements
The compound
Dependencies are inferred from the claim text.