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ID: ALA1133814
Journal: Bioorg Med Chem Lett
Title: Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.
Authors: Zhang P, Terefenko EA, Wrobel J, Zhang Z, Zhu Y, Cohen J, Marschke KB, Mais D.
Abstract: Novel 6-aryl benzimidazolones and benzothiazolones were prepared and examined as bioisosteres of the recently reported 6-aryl dihydroquinolines (1) for progesterone receptor (PR) antagonist activities. PR antagonist activities increased when compounds 9c-f possessed a more lipophilic group at position-1 and pendent aryl moiety para to NH moiety. Furthermore, conversion of carbonyl moiety of 9e,f to the thio-carbonyl led to benzoimidazolethiones 15a,b with significantly improved potency and binding affinity.
CiteXplore: 11591515