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Volumn 21, Issue 17, 2013, Pages 5261-5270
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Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4- yl}propan-2-ol: A novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor
a
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Author keywords
Aldo keto reductase 1C3 (AKR1C3); Castration resistant prostate cancer (CRPC); Testosterone; Type 5 17 hydroxysteroid dehydrogenase (17 HSD5)
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Indexed keywords
1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERIDIN 4 YL METHANOL;
1 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 4 YL] 2 METHYL PROPAN 2 OL;
1 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 4 YL]ACETONE;
1 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 4 YL]PROPAN 2 OL;
2 [1 (1H INDOL 2 YLCARBONYL)AZETIDIN 3 YL]ETHANOL;
2 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 2 YL]ETHANOL;
2 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 3 YL]ETHANOL;
2 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 4 YL] 1 METHOXYETHANE;
2 [1 (1H INDOL 2 YLCARBONYL)PIPERIDIN 4 YL]ETHANOL;
2 [1 (1H INDOL 2 YLCARBONYL)PYRROLIDIN 3 YL]ETHANOL;
2 [1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERAZIN 4 YL]ETHANOL;
2 [1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERIDIN 4 YL]ETHANOL;
2 METHYL 1 [1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERIDIN 4 YL]PROPAN 2 OL;
3 [1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERIDIN 4 YL]PROPANOL;
[1 [(5 METHYL 1H INDOL 2 YL)CARBONYL]PIPERIDIN 4 YL]ACETIC ACID;
ANDROSTENEDIONE;
CYTOCHROME;
OXIDOREDUCTASE INHIBITOR;
POTASSIUM CHANNEL HERG;
REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE;
TESTOSTERONE;
TESTOSTERONE 17BETA DEHYDROGENASE;
TESTOSTERONE 17BETA DEHYDROGENASE TYPE 5;
UNCLASSIFIED DRUG;
ANIMAL EXPERIMENT;
ANIMAL MODEL;
ANIMAL TISSUE;
AREA UNDER THE CURVE;
ARTICLE;
CANCER TISSUE;
CASTRATION;
CHEMICAL MODIFICATION;
CONTROLLED STUDY;
DISTRIBUTION VOLUME;
DRUG BLOOD LEVEL;
DRUG CLEARANCE;
DRUG HALF LIFE;
DRUG IDENTIFICATION;
DRUG POTENCY;
DRUG RESEARCH;
DRUG SELECTIVITY;
DRUG SOLUBILITY;
DRUG STRUCTURE;
DRUG SYNTHESIS;
ENZYME INHIBITION;
HIGH PERFORMANCE LIQUID CHROMATOGRAPHY;
HIGH THROUGHPUT SCREENING;
HORMONE INHIBITION;
HUMAN;
HUMAN CELL;
IC 50;
IN VITRO STUDY;
IN VIVO STUDY;
MALE;
MAXIMUM PLASMA CONCENTRATION;
MOUSE;
NONHUMAN;
PHYSICAL CHEMISTRY;
PROSTATE CANCER;
STRUCTURE ACTIVITY RELATION;
TANDEM MASS SPECTROMETRY;
TESTOSTERONE SYNTHESIS;
TIME TO MAXIMUM PLASMA CONCENTRATION;
TUMOR XENOGRAFT;
MUS MUSCULUS;
ALDO-KETO REDUCTASE 1C3 (AKR1C3);
CASTRATION-RESISTANT PROSTATE CANCER (CRPC);
TESTOSTERONE;
TYPE 5 17Β-HYDROXYSTEROID DEHYDROGENASE (17Β-HSD5);
3-HYDROXYSTEROID DEHYDROGENASES;
ADMINISTRATION, ORAL;
ANIMALS;
DISEASE MODELS, ANIMAL;
DRUG EVALUATION, PRECLINICAL;
ENZYME INHIBITORS;
HALF-LIFE;
HEK293 CELLS;
HUMANS;
HYDROXYPROSTAGLANDIN DEHYDROGENASES;
INDOLES;
MALE;
MICE;
MICE, NUDE;
PIPERIDINES;
PROSTATIC NEOPLASMS;
RATS;
RATS, SPRAGUE-DAWLEY;
STRUCTURE-ACTIVITY RELATIONSHIP;
TESTOSTERONE;
TRANSPLANTATION, HETEROLOGOUS;
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EID: 84881373109
PISSN: 09680896
EISSN: 14643391
Source Type: Journal
DOI: 10.1016/j.bmc.2013.06.025 Document Type: Article |
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Times cited : (10)
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References (20)
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