Molecular Interactions of New Pregnenedione Derivatives
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概要
- 論文の詳細を見る
The in vitro inhibitory activity of five new progesterone derivatives : 17α-hydroxy-16β-methylpregna-1, 4, 6-triene-3, 20-dione 1 ; 16β-methyl-17α-toluoyloxypregna-l, 4, 6-triene-3, 20-dione 2 ; 17α-hydroxy-6-methylenepregn-4-ene-3, 20-dione 3 ; 6-methylene-17α-toluoyloxypregn-4ene-3, 20-dione 4 and 17α- (p-bromobenzoyloxy) -6-methyl-enepregn-4-ene-3, 20-dione 5 was determined. These compounds were evaluated as 5α-reductase inhibitors as well as antagonists for the androgen receptor. Compounds 1, 2, 3, 4 and 5 showed the following inhibitory activity for the 5α-reductase enzyme with IC_<50> values of : 1 (1.65μM), 2 (10μM), 3 (19nM), 4 (100nM) and 5 (100nM). The results of this study also showed the effect of increasing concentrations of the novel steroids upon [^3H] dihydrotestosterone binding to androgen receptors from male hamster prostate. The K_i values for compounds 1, 2, 3, 4, 5 and dihydrotestosterone showed the following order of affinity for the androgen receptor : 4>5>dihydrotestosterone>2>3>1. The overall data indicated that all synthesized compounds 1, 2, 3, 4 and 5 are inhibitors of the 5α-reductase enzyme present in the hamster prostate. In addition compounds 1, 2, 3, 4 and 5 also presented an affinity for the androgen receptor.
- 公益社団法人日本薬学会の論文
- 2003-10-01
著者
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Sanchez Mauricio
Department Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Ramirez Elena
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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BRATOEFF Eugene
Departamento de Farmacia, Facultad de Quimica, UNAM, Ciudad Universitaria
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CABEZA Marisa
Departamento de Farmacia, Facultad de Quimica, UNAM, Ciudad Universitaria
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Flores Eugenio
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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Bratoeff Eugene
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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Valencia Norma
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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Cabeza M
Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Cabeza Marisa
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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HEUZE Ivonne
Departments of Biological Systems and Animal Production, Metropolitan University-Xochimilco
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Heuze Ivonne
Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Ramirez Elena
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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Bratoeff Eugene
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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Sanchez Mauricio
Departamento De Biologia Molecular Y Biotecnologia Instituto De Investigaciones Biomedicas Universidad Nacional Autonoma De Mexico (unam)
関連論文
- Crystal Structure and Synthesis of 17α-(5-Chlorovaleroyloxy)-16β-methylpregna-4,6-diene-3,20-dione
- Crystal Structure and Synthesis of 17α-Acetoxy-4-bromopregn-4-ene-3, 20-dione
- Crystal Structure and Synthesis of 17α-Hexanoyloxy-16β-methylpregna-4,6-diene-3,20-dione
- Crystal Structure and Synthesis of 17α-(5-Bromovalerayloxy)-16β-methylpregna-4,6-diene-3,20-dione
- Crystal Structure of 17-β-Benzoyloxy-16-β-methylpregna-4,6-diene-3,20-dione
- Crystal Stucture of 17α-Acetoxy-6-chloro-16β-methyl-4, 6-pregnadiene-3, 20-dione
- Synthesis and Pharmacological Evaluation of New Progesterone Esters as 5α-Reductase Inhibitors
- Novel 17 Substituted Pregnadiene Derivatives as 5α-Reductase Inhibitors and Their Binding Affinity for the Androgen Receptor
- Molecular Interactions of New Pregnenedione Derivatives
- 5α-Reductase Inhibitory and Antiandrogenic Activities of Novel Steroids in Hamster Seminal Vesicles
- Synthesis and Pharmacological Evaluation of New 16-Methyl Pregnane Derivatives
- New Progesterone Esters as 5α-Reductase Inhibitors
- Evaluation of New Pregnane Derivatives as 5α-Reductase Inhibitor
- Synthesis and Pharmacological Evaluation of 4-Halo Progesterone Derivatives as Antiandrogen
- Antiandrogenic Effect of 16-Substituted, Non-substituted and D-Homopregnane Derivatives
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