Bioactivation of the selective estrogen receptor modulator desmethylated arzoxifene to quinoids: 4′-fluoro substitution prevents quinoid formation

Keyphrases

• 2′-Deoxyguanosine 4%
• Active Form 4%
• Alkaline Phosphatase Activity 4%
• Anti-estrogenic Activity 9%
• Arzoxifene 100%
• Bioactivation 100%
• Breast Cancer Prevention 4%
• Breast Cancer Treatment 9%
• Clinical Trials 4%
• Deoxynucleosides 4%
• Diquinone 31%
• DNA Damage 9%
• Dose Effect 4%
• Electrophilic 9%
• Endometrial Cancer 4%
• Estradiol 4%
• Estrogen Receptor Binding 4%
• Fluorinated Derivatives 4%
• Fluoro-substitution 100%
• Glutathione 4%
• GSH Adduct 4%
• GSH Conjugate 22%
• Human Breast Cancer Cell Lines 4%
• Human Liver Microsomes 4%
• Incubation 9%
• Ishikawa Cells 4%
• Low Activity 4%
• Metabolism 4%
• Methide 31%
• Microsomal Incubation 4%
• O-quinone 4%
• Physiological pH 4%
• Physiological Temperature 4%
• Quinoid 100%
• Raloxifene 13%
• Rat Liver Microsomes 4%
• Receptor Binding Affinity 4%
• Redox-active 4%
• Selective Estrogen Receptor Modulators 100%
• Toxicity in Vivo 4%

Pharmacology, Toxicology and Pharmaceutical Science

• Alkaline Phosphatase 4%
• Arzoxifene 100%
• Bioactivation 100%
• Breast Cancer 13%
• Clinical Trial 4%
• Deoxyguanosine 4%
• Diethylstilbestrol 4%
• Endometrium Cancer 4%
• Estrogen Receptor 4%
• Glutathione 4%
• Quinone Derivative 4%
• Raloxifene 13%
• Selective Estrogen Receptor Modulator 100%
• Tamoxifen 9%