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Literature summary for 1.14.14.32 extracted from

  • Ivanyi, Z.; Woelfling, J.; Goerbe, T.; Szecsi, M.; Wittmann, T.; Schneider, G.
    Synthesis of regioisomeric 17beta-N-phenylpyrazolyl steroid derivatives and their inhibitory effect on 17alpha-hydroxylase/C(17,20)-lyase (2010), Steroids, 75, 450-456.
    View publication on PubMed
Search for more literature for 1.14.14.32

Application

Application Comment Organism
drug development regioisomeric 17beta-N-phenylpyrazolyl steroid derivatives have weak inhibitory effect on 17alpha-hydroxylase/C17,20-lyase Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-4-en-3-one 91% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-5-en-3beta-ol 74% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-chlorophenyl-5-pyrazolyl)androst-4-en-3-one 78% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-chlorophenyl-5-pyrazolyl)androst-5-en-3beta-ol
-
 Rattus norvegicus
17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one 34% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-5-en-3beta-ol
-
 Rattus norvegicus
17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-4-en-3-one 69% relative conversio at 0.05 mMn Rattus norvegicus
17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-5-en-3beta-ol
-
 Rattus norvegicus
17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-4-en-3-one 54% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-5-en-3beta-ol 95% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-4-en-3-one 91% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-5-en-3beta-ol
-
 Rattus norvegicus
17beta-(1-p-tolyl-3-pyrazolyl)androst-4-en-3-one 92% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-tolyl-5-pyrazolyl)androst-4-en-3-one 86% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-tolyl-5-pyrazolyl)androst-5-en-3beta-ol 89% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-tolylphenyl-3-pyrazolyl)androst-5-en-3beta-
-
 Rattus norvegicus
17beta-(1-p-tolylphenyl-3-pyrazolyl)androst-5-en-3beta-ol 93% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-p-tolylphenyl-5-pyrazolyl)androst-5-en-3beta-
-
 Rattus norvegicus
17beta-(1-phenyl-3-pyrazolyl)androst-4-en-3-one 86% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-phenyl-3-pyrazolyl)androst-5-en-3beta-ol 65% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-phenyl-5-pyrazolyl)androst-4-en-3-one 87% relative conversion at 0.05 mM Rattus norvegicus
17beta-(1-phenyl-5-pyrazolyl)androst-5-en-3beta-ol 92% relative conversion at 0.05 mM Rattus norvegicus
ketoconazole
-
 Rattus norvegicus
additional information C17,20-lyase activity is not inhibited by 0.05 mM 17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-5-en-3beta-ol, 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-5-en-3beta-ol, 17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-5-en-3beta-ol and 17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-5-en-3beta-ol; inhibitory effects of synthesized 3beta-hydroxy-17beta-exo-heterocyclic steroids and the corresponding DELTA4-3-ketosteroids on the testicular C17,20-lyase activity are analyzed by an in vitro radioligand incubation technique, overview Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
17alpha-hydroxylase/C(17,20)-lyase
-
 Rattus norvegicus
17alpha-hydroxylase/C17,20-lyase
-
 Rattus norvegicus
P45017alpha
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00035
-
-
 Rattus norvegicus ketoconazole
0.022
-
-
 Rattus norvegicus 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one
0.022
-
 pH and temperature not specified in the publication Rattus norvegicus 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one
0.059
-
-
 Rattus norvegicus 17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-4-en-3-one
0.059
-
 pH and temperature not specified in the publication Rattus norvegicus 17beta-(1-phenyl-5-pyrazolyl)androst-4-en-3-one