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

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...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2001, Vol.49(4), pp.501-503
Hauptverfasser:	EBISAWA, Masayuki, OHTA, Kiminori, KAWACHI, Emiko, FUKASAWA, Hiroshi, HASHIMOTO, Yuichi, KAGECHIKA, Hiroyuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Benzoates - chemistry bioisoster Biological and medical sciences cell differentiation Cell Differentiation - drug effects Drug Synergism General aspects HL-60 Cells Humans Isomerism Medical sciences Pharmacology. Drug treatments Receptors, Retinoic Acid - drug effects retinoid Retinoid X Receptors Retinoids - chemistry Transcription Factors - drug effects tropolone Tropolone - chemistry
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Zusammenfassung:	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).
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.49.501