Finding the Ajoene Sweet‐Spot: Structure‐Activity Relations that Govern its Blood Stability and Cancer Cytotoxicity
Daniel A. Kusza,
Gerhard A. Venter,
Mandla Mabunda
et al.
Abstract:Ajoene is an organosulfur compound found in crushed garlic, that exerts its anti‐cancer activity by S‐thiolating cysteine residues on proteins. Its development is hampered due to limited bioavailability. In this study, we synthesised analogues of ajoene to probe the significance of the ajoene vinyl disulfide/sulfoxide core with respect to cytotoxicity and blood stability. Polar side groups were also incorporated to improve aqueous solubility. It was found that derivatives containing a vinyl disulfide functiona… Show more
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