Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.

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Kikuchi K, Hibi S, Yoshimura H, Tokuhara N, Tai K, Hida T, Yamauchi T, Nagai M

Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.

J Med Chem. 2000 Feb 10;43(3):409-19.

PubMed ID

10669568 [ View in PubMed

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Abstract

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 RARalpha receptor and exerted highly potent cell-differentiating activity on HL-60 cells.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tamibarotene	Retinoic acid receptor alpha	IC 50 (nM)	78	N/A	N/A	Details