| Retinoids have been widely used in the treatment of many diverse diseases including cancers arid skin disorders. Structural modifications of retinoids hold a great potential for discovering new drugs. Unique properties of fluorinated compounds make fluorine substitution a powerful tool for pharmaceutical sciences. Accordingly, this dissertation focuses on the synthesis and biological evaluation of new retinoid derivatives especially fluorinated ones.A series of new retinoids derivatives2,3,4,5,6were designed according to Targretin, one of the most successful medicines in retinoid family. The target compounds2,3,4,5were efficiently synthesized in a divergent way, which is applicable to syntheses of similar retinoid derivatives. Furthermore, biological testing revealed that compounds2,3,4,5could efficiently induce the differentiation of HL-60cells. The IC50values of fluorinated compounds3and5were even lower than that of commercial medicine ATRA. It indicated their great potential in pharmaceutical applications. |
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