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

…, Z Zhang, Y Zhu, J Cohen, KB Marschke, D Mais

Index: Zhang, Puwen; Terefenko, Eugene A.; Wrobel, Jay; Zhang, Zhiming; Zhu, Yuan; Cohen, Jeffrey; Marschke, Keith B.; Mais, Dale Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 20 p. 2747 - 2750

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Citation Number: 39

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 ...