Potent retinoid synergists with a diphenylamine skeleton.
4-[N-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)amino]benzoic acid (5) exhibited weak retinoidal and retinoid synergistic activities in HL-60 cell differentiation assay. N-Alkylation of 5 caused decrease or loss of differentiation-inducing activity, but enhanced the synergistic activity with a synthetic retinoid Am80 (2), as reflected in the potent synergistic EC50 (SEC50) values of DA023 (11, 1.6 x 10(-10) M) and DA113 (14, 1.4 x 10(-10) M) in the presence of 1.0 x 10(-10) M Am80 (2).
Ohta
K
K
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan.
Tsuji
M
M
Kawachi
E
E
Fukasawa
H
H
Hashimoto
Y
Y
Shudo
K
K
Kagechika
H
H
D002454:Cell Differentiation / Q000187:drug effects; D004159:Diphenylamine / Q000494:pharmacology*; D004357:Drug Synergism; D018922:HL-60 Cells; D006801:Humans; D012176:Retinoids / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D012176:Retinoids; D004159:Diphenylamine