Novel retinoidal tropolone derivatives. Bioisosteric relationship of tropolone ring with benzoic acid moiety in retinoid structure

Chemical & Pharmaceutical Bulletin
M EbisawaHiroyuki Kagechika

Abstract

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).

Citations

Jan 5, 2010·Chemical & Pharmaceutical Bulletin·Ai ItoKoichi Shudo
Aug 2, 2005·Clinica Chimica Acta; International Journal of Clinical Chemistry·Mi-Sun KimJin Ho Chung
Dec 7, 2016·Journal of Medical Virology·Bao Ngoc NguyenMasatoshi Hagiwara
Dec 17, 2008·Organic & Biomolecular Chemistry·Victoria B ChristieAndrew Whiting
Feb 3, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Erika CioneFabrizio Manetti
Sep 16, 2005·Journal of Medicinal Chemistry·Hiroyuki Kagechika, Koichi Shudo

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