Substituted ajoenes as novel anti-cancer agents

…, CH Kaschula, IM Parker, MR Caira, P Richards…

Index: Hunter, Roger; Kaschula, Catherine H.; Parker, Iqbal M.; Caira, Mino R.; Richards, Philip; Travis, Susan; Taute, Francois; Qwebani, Thozama Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5277 - 5279

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Citation Number: 29

Abstract

A new synthesis of the ajoene pharmacophore core is presented involving the regioselective radical addition of a thiyl radical to a terminal alkyne as the key step. The synthesis allows structural variation of the two end groups on sulfur, and a range of novel derivatives varying the R1 group (sulfoxide end) has been prepared and tested against CT-1 transformed fibroblast cells for anti-cancer activity. The results indicate comparable or even improved ...