Synthesis of Two Estradiol-Imidazole C-Ribonucleoside Hybrid Compounds Exhibiting Inhibitory Effects against Type 1 17β-Hydroxysteroid Dehydrogenase
摘要:
Novel estradiol-imidazole C-nucleoside hybrid compounds 4a and 4b, which have C4-linked C-0- and C-2-imidazole ribonucleosides as adenosine mimics and amide bond linkers, were designed and synthesized based on EM-1745, an inhibitor of type 1 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD1). Compounds 4a and 4b were also tested as enzyme inhibitors.