The discovery of the potency-enhancing effect of 5-substitutions on the nov
el 2-arylindoles as nonpeptidyl GnRH receptor antagonists led to the identi
fication of several analogues with high affinities on the GnRH receptor. Th
e syntheses and SARs of these 5-substituted-2-arylindole analogues are repo
rted. (C) 2001 Elsevier Science Ltd. All rights reserved.