Potent Retinoid Synergists with a Diphenylamine Skeleton.

Kiminori Ohta, Motonori Tsuji, Emiko Kawachi, Hiroshi Fukasawa, Yuichi HASHIMOTO, Koichi SHUDO, Hiroyuki Kagechika

Biological and Pharmaceutical Bulletin · 1998 · 24 citations · 0 references

DOIFull text

Open access

Concepts

Abstract

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).