Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3, 5, 5, 8, 8-pentamethyl-5, 6, 7, 8- …

…, I Kaneko, J Yang, JS Bhogal, JC Swierski…

Index: Jurutka, Peter W.; Kaneko, Ichiro; Yang, Joanna; Bhogal, Jaskaran S.; Swierski, Johnathon C.; Tabacaru, Christa R.; Montano, Luis A.; Huynh, Chanh C.; Jama, Rabia A.; Mahelona, Ryan D.; Sarnowski, Joseph T.; Marcus, Lisa M.; Quezada, Alexis; Lemming, Brittney; Tedesco, Maria A.; Fischer, Audra J.; Mohamed, Said A.; Ziller, Joseph W.; Ma, Ning; Gray, Geoffrey M.; Van Der Vaart, Arjan; Marshall, Pamela A.; Wagner, Carl E. Journal of Medicinal Chemistry, 2013 , vol. 56, # 21 p. 8432 - 8454

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Citation Number: 5

Abstract

Three unreported analogues of 4-[1-(3, 5, 5, 8, 8-pentamethyl-5-6-7-8-tetrahydro-2-naphthyl) ethynyl] benzoic acid (1), otherwise known as bexarotene, as well as four novel analogues of (E)-3-(3-(1, 2, 3, 4-tetrahydro-1, 1, 4, 4, 6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl) acrylic acid (CD3254), are described and evaluated for their retinoid X receptor (RXR) selective agonism. Compound 1 has FDA approval as a treatment for cutaneous T-cell ...