Abstract
CYP17 inhibition is a promising therapy for prostate cancer (PC) because proliferation of 80% of PC depends on androgen stimulation. Introduction of isopropylidene substituents onto the linker of biphenylmethylene 4-pyridines resulted in several strong CYP17 inhibitors, which were more potent and selective, regarding CYP 11B1, 11B2, 19 and 3A4, than the drug candidate abiraterone.
MeSH terms
-
Antineoplastic Agents, Hormonal / chemical synthesis
-
Antineoplastic Agents, Hormonal / chemistry
-
Antineoplastic Agents, Hormonal / metabolism
-
Biphenyl Compounds / chemical synthesis
-
Biphenyl Compounds / chemistry
-
Biphenyl Compounds / metabolism
-
Biphenyl Compounds / pharmacology*
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / metabolism
-
Enzyme Inhibitors / pharmacology*
-
Humans
-
Inhibitory Concentration 50
-
Magnetic Resonance Spectroscopy
-
Male
-
Neoplasms, Hormone-Dependent / drug therapy
-
Neoplasms, Hormone-Dependent / enzymology
-
Prostatic Neoplasms / drug therapy
-
Prostatic Neoplasms / enzymology
-
Pyridines / chemical synthesis
-
Pyridines / chemistry
-
Pyridines / metabolism
-
Pyridines / pharmacology*
-
Spectrometry, Mass, Electrospray Ionization
-
Steroid 17-alpha-Hydroxylase / antagonists & inhibitors*
-
Steroid 17-alpha-Hydroxylase / metabolism
-
Structure-Activity Relationship
-
Substrate Specificity
Substances
-
Antineoplastic Agents, Hormonal
-
Biphenyl Compounds
-
Enzyme Inhibitors
-
Pyridines
-
Steroid 17-alpha-Hydroxylase