1218
K. Kikuchi et al. / Bioorg. Med. Chem. Lett. 11 (2001) 1215–1218
on cell differentiation, and possessed selective affinity
for RARa receptor. Furthermore, 12f did not have
transactivation activity for any receptor subtype, and it
showed RARa-selective antagonistic activity.
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Roberts, A. B., Goodman, D. S., Eds.; Raven: New York,
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son, M. I. Toxicol. Appl. Pharmacol. 1990, 103, 324.
In conclusion, novel benzoic acid derivatives which have
an 8-isopropylquinoline moiety in the hydrophobic part
and 2,5-disubstituted pyrrole moiety in the linking part
possessed RARa selectivity. One of them, 4-[5-[8-(1-
methylethyl)-4-phenyl-2-quinolinyl]-1H-2-pyrrolyl]ben-
zoic acid (12f: ER-50891) showed potent RARa-selec-
tive antagonistic activity. This antagonist could be
useful in studies of the role of the RARa receptor in the
action of retinoids, and might be a useful lead compound
for drugs to treat diseases caused by RARa-mediated
gene transactivation.
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