Highly twisted adamantyl arotinoids: synthesis, antiproliferative effects and RXR transactivation profiles

…, R Pereira, F Rodríguez-Barrios, ÁR de Lera…

Index: Perez-Rodriguez, Santiago; Ortiz, Maria A.; Pereira, Raquel; Rodriguez-Barrios, Fatima; de Lera, Angel R.; Piedrafita, F. Javier European Journal of Medicinal Chemistry, 2009 , vol. 44, # 6 p. 2434 - 2446

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Citation Number: 8

Abstract

Retinoid-related molecules with an adamantyl group (adamantyl arotinoids) have been described with selective activities towards the retinoid receptors as agonists for NR1B2 and NR1B3 (RARβ, γ)(CD437, MX3350-1) or RAR antagonists (MX781) that induce growth arrest and apoptosis in cancer cells. Since these molecules induce apoptosis independently of RAR transactivation, we set up to synthesize novel analogs with impaired RAR binding. ...