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  • Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.

Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.

Bioorganic & medicinal chemistry letters (2001-10-10)
P Zhang, E A Terefenko, J Wrobel, Z Zhang, Y Zhu, J Cohen, K B Marschke, D Mais
PMID11591515
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.