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2-Alkylsulfanyl estrogen derivatives: synthesis of a novel class of multi-targeted anti-tumour agents


Reference:

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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Official URL:

http://dx.doi.org/10.1016/j.bmcl.2004.04.027

Abstract

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.

Details

Item Type Articles
CreatorsLeese, M. P., Newman, S. P., Purohit, A., Reed, M. J. and Potter, B. V. L.
DOI10.1016/j.bmcl.2004.04.027
DepartmentsFaculty of Science > Pharmacy & Pharmacology
RefereedYes
StatusPublished
ID Code8060

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