Novel Retinoidal Tropolone Derivatives. Bioisosteric Relationship of Tropolone Ring with Benzoic Acid Moiety in Retinoid Structure

Masayuki EBISAWA; Kiminori OHTA; Emiko KAWACHI; Hiroshi FUKASAWA; Yuichi HASHIMOTO; Hiroyuki KAGECHIKA

doi:10.1248/cpb.49.501

Communications to the Editor

Novel Retinoidal Tropolone Derivatives. Bioisosteric Relationship of Tropolone Ring with Benzoic Acid Moiety in Retinoid Structure

Masayuki EBISAWA, Kiminori OHTA, Emiko KAWACHI, Hiroshi FUKASAWA, Yuichi HASHIMOTO, Hiroyuki KAGECHIKA

著者情報

キーワード: retinoid, tropolone, bioisoster, cell differentiation

ジャーナルフリー

2001 年 49 巻 4 号 p. 501-503

DOI https://doi.org/10.1248/cpb.49.501

詳細

抄録

Several tropolone derivatives (4-7) were designed as novel retinoids on the assumption that the tropolone ring may mimic the benzoic acid moiety in retinoid structures, such as Am80 (2). Among the synthesized compounds, 5-[2-(5, 6, 7, 8-tetrahydro-5, 5, 8, 8-tetramethyl-2-naphthyl)ethynyl]tropolone (7a) showed moderate potency as a differentiation-inducer of HL-60 cells. The activities of the tropolones were greatly enhanced in the presence of HX630, an RXR agonist (retinoid synergist).

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