Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a series of 4-hydroxyphenyl ketones as potential inhibitors of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3)

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 17, 2006, Pages 4519-4522

  Lota, Rupinder K ^a   Dhanani, Sachin ^a   Owen, Caroline P ^a   Ahmed, Sabbir ^a  

^a KINGSTON UNIVERSITY   (United Kingdom)

Author keywords

17 hydroxysteroid dehydrogenase; Androstenedione; Inhibitors; Testosterone; Type 3

Indexed keywords

1 (4 HYDROXYPHENYL)NONAN 1 ONE; 17BETA HYDROXYSTEROID DEHYDROGENASE 3 INHIBITOR; 7 HYDROXYFLAVONE; ANDROSTENEDIONE; BAICALEIN; KETONE DERIVATIVE; OXIDOREDUCTASE INHIBITOR; TESTOSTERONE; TESTOSTERONE 17BETA DEHYDROGENASE; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL ANALYSIS; DRUG ACTIVITY; DRUG POTENCY; DRUG SYNTHESIS; IC 50;

17-HYDROXYSTEROID DEHYDROGENASES; CATALYSIS; HYDROGEN; KETONES; MODELS, MOLECULAR; MOLECULAR STRUCTURE;

EID: 33746206218     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.06.029     Document Type: Article

References (10)

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5. 2 requires C, 70.58%; H, 5.92%.
6. 2 requires C, 71.98%, H, 6.71%.
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8. 50 was then determined from a graph (using linear regression analysis) of the inhibitory activity versus log [I].
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10. Quantum Cache Project Leader is a trademark of Oxford Molecular Ltd (Fujitsu), Oxford Science Park, Oxford, UK.