2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents
Leese, M. P., Newman, S. P., Purohit, A., Reed, M. J. and Potter, B. V. L., 2004. 2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents. Bioorganic & Medicinal Chemistry Letters, 14 (12), pp. 3135-3138.
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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. (C) 2004 Elsevier Ltd. All rights reserved.
|Creators||Leese, M. P., Newman, S. P., Purohit, A., Reed, M. J. and Potter, B. V. L.|
|Departments||Faculty of Science > Pharmacy & Pharmacology|
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