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

M P Leese, S P Newman, A Purohit, M J Reed, B V L Potter

Research output: Contribution to journalArticle

31 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)3135-3138
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume14
Issue number12
DOIs
Publication statusPublished - 2004

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Steryl-Sulfatase
Estrone
Tumors
Estradiol
Estrogens
Display devices
Hormones
Derivatives
Enzymes
Neoplasms
sulfamic acid
2-methoxyestradiol

Cite this

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; Potter, B V L.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 14, No. 12, 2004, p. 3135-3138.

Research output: Contribution to journalArticle

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