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A flexible, direct, high yielding synthesis of 2-alkylsulfanyl estrogens from estrone has been developed. 2-Methylsulfanyl estradiol (2-MeSE2) 7 displays a similar anti-proliferative activity to the established 2-methoxyestradiol (2-MeOE2) 1, whilst its 3-O-sulfamate derivative (2-MeSE2MATE) 9 exhibits greatly enhanced anti-proliferative activity, combined with significant inhibition of steroid sulfatase, an enzyme target for the treatment of hormone-dependent tumours.

Original publication

DOI

10.1016/j.bmcl.2004.04.027

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

21/06/2004

Volume

14

Pages

3135 - 3138

Keywords

Antineoplastic Agents, Cell Line, Tumor, Drug Delivery Systems, Estrogens, Humans, Sulfuric Acid Esters