396725-90-9Relevant academic research and scientific papers
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones
Zhang, Puwen,Terefenko, Eugene A.,Wrobel, Jay,Zhang, Zhiming,Zhu, Yuan,Cohen, Jeffrey,Marschke, Keith B.,Mais, Dale
, p. 2747 - 2750 (2007/10/03)
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.
