Small molecule-inhibitors of 6-phosphofructo-1-kinase for reducing Reactive oxygen species (ROS) generation by cancer cells

Small molecule-inhibitors of 6-phosphofructo-1-kinase for reducing Reactive oxygen species (ROS) generation by cancer cells

The present invention relates to a compound selected from the group consisting of: (2-[(5-benzo[1,3]dioxol-5-yl-1,3,4-oxadiazol-2-yl)sulfanyl]-N-isoxazol-3-yl-acetamide) 5 (Inhibitor No. 3); (3-methoxy-6-(3-{1 -[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1 H-pyrazol-3-yl}phenyl)pyridazine) (Inhibitor No...

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Hauptverfasser: MAROLT Nika, LEGISA Matic, SOLMAJER Tomaz, LESNIK Samo, KONC Janez
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HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator MAROLT Nika
LEGISA Matic
SOLMAJER Tomaz
LESNIK Samo
KONC Janez
description The present invention relates to a compound selected from the group consisting of: (2-[(5-benzo[1,3]dioxol-5-yl-1,3,4-oxadiazol-2-yl)sulfanyl]-N-isoxazol-3-yl-acetamide) 5 (Inhibitor No. 3); (3-methoxy-6-(3-{1 -[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1 H-pyrazol-3-yl}phenyl)pyridazine) (Inhibitor No. 9); (4-[3-(5-amino-1,3,4-oxadiazol-2-yl)isoxazol-5-yl]phenol) (Inhibitor No. 30); (N-[5-(methanesulfonamido)-1,3,4-thiadiazol-2-yl]-6,7,8,9-tetrahydro-5H-carbazole-3- 10 carboxamide) (Inhibitor No. 23); (3-(4-chlorophenyl)sulfonyl-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 29); ((2R)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)-2,3-dihydro-1,4-benzodioxine-2-carboxamide) (Inhibitor No. 31); and 15 (3-(benzenesulfonyl)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 32); or a pharmaceutically acceptable salt, solvate or derivative thereof, for use in a method of treatment of a cancer, dysplasia and/or carcinoma in situ through inhibition of ROS generation in the cells of the neoplasm associated with said cancer, dysplasia and/or carcinoma in situ.
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(3-methoxy-6-(3-{1 -[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1 H-pyrazol-3-yl}phenyl)pyridazine) (Inhibitor No. 9); (4-[3-(5-amino-1,3,4-oxadiazol-2-yl)isoxazol-5-yl]phenol) (Inhibitor No. 30); (N-[5-(methanesulfonamido)-1,3,4-thiadiazol-2-yl]-6,7,8,9-tetrahydro-5H-carbazole-3- 10 carboxamide) (Inhibitor No. 23); (3-(4-chlorophenyl)sulfonyl-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 29); ((2R)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)-2,3-dihydro-1,4-benzodioxine-2-carboxamide) (Inhibitor No. 31); and 15 (3-(benzenesulfonyl)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 32); or a pharmaceutically acceptable salt, solvate or derivative thereof, for use in a method of treatment of a cancer, dysplasia and/or carcinoma in situ through inhibition of ROS generation in the cells of the neoplasm associated with said cancer, dysplasia and/or carcinoma in situ.</description><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2023</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFi7EKwjAURbs4iPoNvlGHgLVQnBXFQRBanUv6fGmDaV5IUrH483Zwd7gcOJw7TT5lJ42Bjg1hb0ho2-paR_YBWEEuXMthnPI9RhapeGorA4FiD54ePWrbQEESo34R8HtoyEJwhJoCrIpruYbRkJdRs4V6AJQWyQOSMWGeTJQ0gRY_zpLl6Xg7nAU5rig4ieM1Vpd7utnu8myfZv-LL0GrRe8</recordid><startdate>20230420</startdate><enddate>20230420</enddate><creator>MAROLT Nika</creator><creator>LEGISA Matic</creator><creator>SOLMAJER Tomaz</creator><creator>LESNIK Samo</creator><creator>KONC Janez</creator><scope>EVB</scope></search><sort><creationdate>20230420</creationdate><title>Small molecule-inhibitors of 6-phosphofructo-1-kinase for reducing Reactive oxygen species (ROS) generation by cancer cells</title><author>MAROLT Nika ; 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(3-methoxy-6-(3-{1 -[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-1 H-pyrazol-3-yl}phenyl)pyridazine) (Inhibitor No. 9); (4-[3-(5-amino-1,3,4-oxadiazol-2-yl)isoxazol-5-yl]phenol) (Inhibitor No. 30); (N-[5-(methanesulfonamido)-1,3,4-thiadiazol-2-yl]-6,7,8,9-tetrahydro-5H-carbazole-3- 10 carboxamide) (Inhibitor No. 23); (3-(4-chlorophenyl)sulfonyl-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 29); ((2R)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)-2,3-dihydro-1,4-benzodioxine-2-carboxamide) (Inhibitor No. 31); and 15 (3-(benzenesulfonyl)-N-(5-isoxazol-5-yl-1,3,4-oxadiazol-2-yl)propanamide) (Inhibitor No. 32); or a pharmaceutically acceptable salt, solvate or derivative thereof, for use in a method of treatment of a cancer, dysplasia and/or carcinoma in situ through inhibition of ROS generation in the cells of the neoplasm associated with said cancer, dysplasia and/or carcinoma in situ.</abstract><oa>free_for_read</oa></addata></record>
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subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Small molecule-inhibitors of 6-phosphofructo-1-kinase for reducing Reactive oxygen species (ROS) generation by cancer cells
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