Synthesis and Pharmacological Evaluation of 4-Halo Progesterone Derivatives as Antiandrogen

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概要

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• The pharmacological activity of eight pregnane derivatives 17-α acetoxyprogesterone 9,17-α acetoxy-4,5-epoxypregnan-3,20-dione 10,17-α acetoxy-4-chloro-4-pregnene-3,20-dione 11,17-α acetoxy-4-bromo-4-pregnene-3,20-dione 12,17-α hydroxy-4-bromo-4-pregnene-3,20-dione 13,4-chloro-17-α hydroxy-4-pregnene-3,20-dione 14,17-α benzoyloxy-4-bromo-4-pregnene-3,20-dione 15 and 17-α benzoyloxy-4-chloro-4-pregnene-3,20-dione 16 was aeter, mined. These compounds were evaluated as antiandrogens on gonadectomized hamster seminal vesicles.The pharmacological data in this study indicate that compounds 15 and 16 having a C-17 benzoyloxy moiety showed the highest antiandrogenic activity as measured by the reduction of the weight of the seminal vesicles, followed by the steroids 11 and 12 (17-α acetoxy group). The free alcohols 13 and 14 exhibited a lower antiandrogenic activity. Apparently, the ester moiety at C-17 is a necessary requirement for the presence of high antiandrogenic activity. shows the inhibitory effect on the conversion of testosterone (T) to DHT, of the above described steroids as measured by the amount of produced DHT 2 expressed as pmoles of DHT/g of protein/h.Steroids 11,12 and 16 showed a much higher inhibitory activity on the conversion of testosterone (T) to dihydrotestosterone (DHT) than presently used finasteride 3.

• 公益社団法人日本薬学会の論文
• 1999-09-15

著者

• Ramirez Elena

  Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City

• CABEZA Marisa

  Departamento de Farmacia, Facultad de Quimica, UNAM, Ciudad Universitaria

• FLORES Gregoria

  Departamento de Farmacia, Facultad de Quimica, UNAM

• Quiroz Alexandra

  Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco

• Flores Gregoria

  Departamento De Farmacia Facultad De Quimica Unam

• Bratoeff Eugene

  Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City

• Murillo Ma

  Faculty Of Chemistry National University Of Mexico

• Cabeza M

  Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco

• Cabeza Marisa

  Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria

• BRATOEFF Eugene

  Faculty of Chemistry, National University of Mexico D.F.

• RAMIREZ Elena

  Faculty of Chemistry, National University of Mexico

• FLORES Gregoria

  Faculty of Chemistry, National University of Mexico

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

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