Nucleophilic vinylic 'addition-elimination' substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene: A novel and general route to 17-substituted steroids. Part 1 - Synthesis of novel 17-azolyl-Δ16 steroids; inhibitors of 17α-hydroxylase/17,20-lyase (17α-lyase)

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 22, 1996, Pages 2777-2782

  Njar, Vincent C O ^a,b   Klus, Gregory T ^a   Brodie, Angela M H ^a  

^a UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF IBADAN   (Nigeria)

Author keywords

[No Author keywords available]

Indexed keywords

3BETA HYDROXY 17 (1H IMIDAZOL 1 YL)ANDROSTA 5,16 DIENE; ANDROSTANE DERIVATIVE; LYASE INHIBITOR; STEROID 17,20 LYASE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG SYNTHESIS; ENZYME BINDING; ENZYME INHIBITION; HUMAN; IN VITRO STUDY; NUCLEAR MAGNETIC RESONANCE; REACTION ANALYSIS; SPECTROPHOTOMETRY; TECHNIQUE;

EID: 0030593886     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00512-4     Document Type: Article

References (29)

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27. 2 338.2358, found 338.2361.
28. 50 refers to the inhibitor concentration which produced 50% inhibition of the enzyme activity. The correlation coefficents r > 95% for all tested compounds.
29. 13. The enzyme used was a modified form of human 17α-lyase (CYP 17) which was expressed in E. coli and purified as descibed in Imai, T.; Globerman, H.; Gertner, J. M.; Kagawa, N.; Waterman, M. R. J. Biol. Chem. 1993, 268, 19681.