Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor α agonists

Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (7), p.623-625
Hauptverfasser:	HIBI, S, TAGAMI, K, KIKUCHI, K, YOSHIMURA, H, TAI, K, HIDA, T, TOKUHARA, N, YAMAUCHI, T, NAGAI, M
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Benzoates - chemical synthesis Benzoates - pharmacology Benzopyrans - chemical synthesis Benzopyrans - pharmacology Biological and medical sciences Cell Differentiation - drug effects General aspects HL-60 Cells Humans Medical sciences Naphthalenes - chemical synthesis Naphthalenes - pharmacology Pharmacology. Drug treatments Pyrroles - chemical synthesis Pyrroles - pharmacology Receptors, Retinoic Acid - agonists Retinoic Acid Receptor alpha Structure-Activity Relationship
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Zusammenfassung:	Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activity at the RAR alpha receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00067-6