Practical synthesis of a chromene analog for use as a retinoic acid receptor alpha antagonist lead compound

R Jetson, N Malik, A Luniwal, V Chari, M Ratnam…

Index: Jetson, Rachael; Malik, Neha; Luniwal, Amarjit; Chari, Venkatesh; Ratnam, Manohar; Erhardt, Paul European Journal of Medicinal Chemistry, 2013 , vol. 63, p. 104 - 108

Full Text: HTML

Citation Number: 6

Abstract

Retinoic acid receptor alpha (RARα) selective compounds may guide the design of drugs that can be used in conjunction with hormonal adjuvant therapy in the treatment of breast cancer. Herein we report a modified synthesis of a known RARα antagonist, 2-fluoro-4-[[[8- bromo-2, 2-dimethyl-4-(4-methylphenyl) chroman-6-yl] carbonyl] amino] benzoic acid and a synthesis of its unknown, desfluoro analog, 4-[[[8-bromo-2, 2-dimethyl-4-(4-methylphenyl) ...