PMID: 7539071Jan 1, 1994Paper

Pyridyl substituted benzocycloalkenes: new inhibitors of 17 alpha-hydroxylase/17,20-lyase (P450 17 alpha)

Journal of Enzyme Inhibition
T F Sergejew, Rolf W Hartmann

Abstract

Compounds capable of inhibiting 17 alpha-hydroxylase/17,20-lyase (P450 17 alpha) are of great interest for the therapy of prostatic cancer since they block androgen biosynthesis. In order to evaluate the inhibitory activity of a series of benzocycloalkenes developed in our group, an in vitro assay was established using rat testicular microsomes as source of the enzyme, non labelled progesterone as substrate and a HPLC procedure for separation of the steroids. The inhibitory activities of 33 test compounds were compared to ketoconazole (IC50 67 microM), a known inhibitor of P450 17 alpha, which recently has been successfully used in prostate cancer patients. Several compounds of the present study were stronger inhibitors of P450 17 alpha than ketoconazole. The most active compounds were compound 12(5-methoxy-2-(4-pyridylmethyl)-1-tetralone: IC50 13 microM) and compound 13(5-methoxy-2-(4-pyridyl)-1-tetralone: IC50 13 microM).

References

Dec 1, 1989·Journal of Steroid Biochemistry·S E BarrieM Jarman
Nov 1, 1986·The Journal of Clinical Endocrinology and Metabolism·J RajferD J Handelsman
Jun 1, 1980·Antimicrobial Agents and Chemotherapy·H Van den BosscheJ M van Cutsem
Jul 1, 1984·The Journal of Urology·J Trachtenberg

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Citations

Feb 21, 2002·Archiv der Pharmazie·S HaidarR W Hartmann
Sep 11, 2007·Bioscience, Biotechnology, and Biochemistry·Ken-ichi KimuraMakoto Yoshihama
Nov 6, 2008·Nature Clinical Practice. Urology·Alison Hm ReidJohann S de Bono
Jan 25, 2005·Journal of Enzyme Inhibition and Medicinal Chemistry·Marie-Pierre LézéRolf W Hartmann
Jul 12, 2002·Archiv der Pharmazie·Rolf W HartmannYan Zhuang
May 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·T F Sergejew, R W Hartmann
Feb 12, 2002·Bioorganic & Medicinal Chemistry·Joseph P BurkhartNorton P Peet
Apr 18, 2003·Bioorganic & Medicinal Chemistry Letters·Pascal MarchandRolf W Hartmann

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