Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

Wrobel Tomasz M.; Jorgensen Flemming Steen; Pandey Amit V.Grudzinska AngelikaSharma KatyayaniYakubu JibiraBjorkling Fredrik

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Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

机译：Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

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摘要

CYP17A1 is an enzyme that plays a major role in steroidogenesisand is critically involved in the biosynthesis of steroid hormones.Therefore, it remains an attractive target in several serious hormone-dependentcancer diseases, such as prostate cancer and breast cancer. The medicinalchemistry community has been committed to the discovery and developmentof CYP17A1 inhibitors for many years, particularly for the treatmentof castration-resistant prostate cancer. The current Perspective reflectsupon the discovery and evaluation of non-steroidal CYP17A1 inhibitorsfrom a medicinal chemistry angle. Emphasis is placed on the structuralaspects of the target, key learnings from the presented chemotypes,and design guidelines for future inhibitors.

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《Journal of Medicinal Chemistry》 |2023年第10期|6542-6566|共25页
作者
Wrobel Tomasz M.; Jorgensen Flemming Steen; Pandey Amit V.Grudzinska AngelikaSharma KatyayaniYakubu JibiraBjorkling Fredrik;
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作者单位

Med Univ Lublin;

Univ Copenhagen;

Univ Childrens Hosp;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
CHROMATOGRAPHY-MASS-SPECTROMETRY; IMIDAZOLE-BASED COMPOUNDS; HUMAN 17-ALPHA-HYDROXYLASE-17; 20-LYASE CYP17; RESISTANT PROSTATE-CANCER; HUMAN CYTOCHROME P450C17; BIOCHEMICAL EVALUATION; BIOLOGICAL EVALUATION; ANDROGEN RECEPTOR; HIGHLY POTENT; C-17; C-20-LYASE INHIBITORS;

Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

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