title: Synthesis and screening of aromatase inhibitory activity of substituted C19 steroidal 17-oxime analogs.
abstract: The synthesis and aromatase inhibitory activity of androst-4-en-, androst-5-en-, 1β,2β-epoxy- and/or androsta-4,6-dien-, 4β,5β-epoxyandrostane-, and 4-substituted androst-4-en-17-oxime derivatives are described. Inhibition activity of synthesized compounds was assessed using aromatase enzyme and [1β-3H]androstenedione as substrate. Most of the compounds displayed similar to or more aromatase inhibitory activity than formestane (74.2%). 4-Chloro-3β-hydroxy-4-androsten-17-one oxime (14, 93.8%) showed the highest activity, while 4-azido-3β-hydroxy-4-androsten-17-one oxime (17, 32.8%) showed the lowest inhibitory activity for aromatase.
authors: College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea.
authors: Muna
authors: M
authors: Pokhrel
authors: Eunsook
authors: E
authors: Ma
mesh_terms: D001141:Aromatase / Q000378:metabolism; D047072:Aromatase Inhibitors / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010091:Oximes / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013256:Steroids / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D047072:Aromatase Inhibitors; D010091:Oximes; D013256:Steroids; D001141:Aromatase