Syntheses and Structure−Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor α Agonistic Activity

In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of quinoxaline derivatives. One of them, 4-[5-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxalinyl)-1H-2-pyrrolyl]benzoic acid (3a), which possesses a 2,5-disubstituted pyrrole moiety,...

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Veröffentlicht in:	Journal of medicinal chemistry 2000-02, Vol.43 (3), p.409-419
Hauptverfasser:	Kikuchi, Kouichi, Hibi, Shigeki, Yoshimura, Hiroyuki, Tokuhara, Naoki, Tai, Kenji, Hida, Takayuki, Yamauchi, Toshihiko, Nagai, Mitsuo
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Benzoates - chemical synthesis Benzoates - chemistry Benzoates - metabolism Benzoates - pharmacology Binding, Competitive Biological and medical sciences Cell Differentiation - drug effects Cell Line General aspects Humans Medical sciences Pharmacology. Drug treatments Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - metabolism Quinoxalines - pharmacology Receptors, Retinoic Acid - agonists Receptors, Retinoic Acid - metabolism Retinoic Acid Receptor alpha Retinoids - chemical synthesis Retinoids - chemistry Retinoids - metabolism Retinoids - pharmacology Structure-Activity Relationship
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Zusammenfassung:	In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of quinoxaline derivatives. One of them, 4-[5-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxalinyl)-1H-2-pyrrolyl]benzoic acid (3a), which possesses a 2,5-disubstituted pyrrole moiety, showed selectivity for the RARα receptor and exerted highly potent cell-differentiating activity on HL-60 cells.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm990063w