3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1

4-(3-(4-( N-Methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate ( 11k) is a competitive 5α-reductase inhibitor with the IC 50 value of 0.84 μM. We designed and synthesized novel type 1 5α-reductase inhibitors by using 3,3-diphenylpentane skeleton as a substitute for the usual steroid skeleto...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 19; pp. 5414 - 5418
Main Authors Hosoda, Shinnosuke, Hashimoto, Yuichi
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 01.10.2007
Elsevier
Subjects
3,3-Diphenylpentane
5α-Reductase
Antineoplastic agents
Biological and medical sciences
General aspects
Inhibitor
Medical sciences
Pharmacology. Drug treatments
Steroid
Steroid
Inhibitor
3,3-Diphenylpentane
5α-Reductase
Antineoplastic agent
Human
Enzyme
Benzene derivatives
Enzyme inhibitor
In vitro
Structure activity relation
Carboxamide
Oxidoreductases
Chemical synthesis
Non steroid compound
3-Oxo-5α-steroid 4-dehydrogenase
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Summary:4-(3-(4-( N-Methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate ( 11k) is a competitive 5α-reductase inhibitor with the IC 50 value of 0.84 μM. We designed and synthesized novel type 1 5α-reductase inhibitors by using 3,3-diphenylpentane skeleton as a substitute for the usual steroid skeleton. 4-(3-(4-( N-Methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate ( 11k) is a competitive 5α-reductase inhibitor with the IC 50 value of 0.84 μM.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.07.039