SYNTHESIS OF TWO ESTRADIOL-IMIDAZOLE C-RIBONUCLEOSIDE HYBRID COMPOUNDS EXHIBITING INHIBITORY EFFECTS AGAINST TYPE 117β-HYDROXYSTEROID DEHYDROGENASE

摘要

Novel estradiol-imidazole C-nucleoside hybrid compounds 4a and 4b, which have C4-linked Co-and C2-imidazole ribonucleosides as adenosine mimics and amide bond linkers, were designed and synthesized based on EM-1745, an inhibitor of type 117β-hydroxysteroid dehydrogenase (17β-HSD1). Compounds 4a and 4b were also tested as enzyme inhibitors.