Novel CYP17 inhibitors: Synthesis, biological evaluation, structure–activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls

Recently, the steroidal CYP17 inhibitor Abiraterone entered phase II clinical trial for the treatment of androgen-dependent prostate cancer. As 17α-hydroxylase-17,20-lyase (CYP17) catalyzes the last step in androgen biosynthesis, inhibition of this target should affect not only testicular but also a...

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Veröffentlicht in:	European journal of medicinal chemistry 2009-07, Vol.44 (7), p.2765-2775
Hauptverfasser:	Hille, Ulrike E., Hu, Qingzhong, Vock, Carsten, Negri, Matthias, Bartels, Marc, Müller-Vieira, Ursula, Lauterbach, Thomas, Hartmann, Rolf W.
Format:	Artikel
Sprache:	eng
Schlagworte:	17α-Hydroxylase-17,20-lyase (CYP17) inhibitors Androgens Antineoplastic agents Biological and medical sciences Biphenyl Compounds - chemical synthesis Biphenyl Compounds - chemistry Biphenyl Compounds - pharmacology Catalytic Domain CYP11B1 CYP3A4 Cytochrome P-450 CYP3A Cytochrome P-450 CYP3A Inhibitors Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Humans Medical sciences Models, Molecular Pharmacology. Drug treatments Prostate cancer Steroid 11-beta-Hydroxylase - antagonists & inhibitors Steroid 17-alpha-Hydroxylase - antagonists & inhibitors Steroid 17-alpha-Hydroxylase - chemistry Steroidomimetics Structure-Activity Relationship Substrate Specificity Urinary system
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