Novel analogs of 3-[4-hydroxy-3-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)phenyl]-2-propenoic acid (CD3254) possessing a pyridine ring were synthesized and evaluated for transcriptional activity in retinoid-X-receptor (RXR) mammalian-2-hybrid (M2H) and RXR-element (RXRE) assays in HCT-116 cells. A range of different transcriptional activities was observed, and the novel target analogs displayed a range of EC50 values. Some novel analogs possessed similar potency as CD3254 and greater potency than 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid (bexarotene), and some novel analogs were far less potent than CD3254 and bexarotene.

Synthesis and biological characterization of novel CD3254 analogs

251st National Meeting (2016)

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