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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Leese MP,Newman SP,Purohit A,Reed MJ,Potter BV

doi

10.1016/j.bmcl.2004.04.027

subject

Has Abstract

pub_date

2004-06-21 00:00:00

pages

3135-8

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960894X04005256

journal_volume

14

pub_type

杂志文章

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