Synthesis and biological evaluation of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitors based on a thieno[2,3-d] pyrimidin-4(3H)-one core

Journal of Medicinal Chemistry

Volumn 52, Issue 21, 2009, Pages 6660-6671

  Lilienkampf, Annamaria ^a   Karkola, Sampo ^a   Alho Richmond, Sari ^a   Koskimies, Pasi ^b   Johansson, Nina ^b   Huhtinen, Kaisa ^b,c   Vihko, Kimmo ^b,c   Wähälä, Kristiina ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

^b Hormos Medical Ltd   (Finland)

^c UNIVERSITY OF TURKU   (Finland)

Author keywords

[No Author keywords available]

Indexed keywords

17BETA HYDROXYSTEROID DEHYDROGENASE TYPE 1; 3,4,9,10,11,12 HEXAHYDRO 1H CYCLOHEPTA[40,50]THIENO[20,30:4,5] PYRIMIDO[1,2 A]AZEPINE 5,14(2H,8H) DIONE; 4 (3 HYDROXYPHENYLTHIO) 1,2,7,8,9,10,11,13 OCTAHYDRO 13 OXO [1]BENZOTHIENO[20,30:4,5]PYRIMIDO[1,2 A]AZEPINE 3 CARBOXALDEHYDE; 6,7 DIHYDRO 3 METHYL [1]BENZOTHIENO[2,3 D]PYRIMIDINE 4,8(3H,5H) DIONE; ESTROGEN RECEPTOR; HORMONE INHIBITOR; PYRIMIDINE DERIVATIVE; TESTOSTERONE 17BETA DEHYDROGENASE; THIENO[2,3 D]PYRIMIDIN 4(3H) ONE; UNCLASSIFIED DRUG;

ARTICLE; BINDING ASSAY; BIOSYNTHESIS; CATALYSIS; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS;

17-HYDROXYSTEROID DEHYDROGENASES; ANTINEOPLASTIC AGENTS; AZEPINES; BREAST NEOPLASMS; CELL LINE, TUMOR; ESTRADIOL DEHYDROGENASES; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTROGENS; FEMALE; HUMANS; ISOENZYMES; MODELS, MOLECULAR; NEOPLASMS, HORMONE-DEPENDENT; PYRIMIDINONES; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 71049157137     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900928k     Document Type: Article

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