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Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.

Abstract：

:2-Alkylchromen-4-one 6-O-sulfamates, a new class of potent steroid sulfatase (STS) inhibitors, were evaluated for their estrogenic potential. Structure-activity relationships for estrogenic activity were identified; however, no correlation with STS inhibition was found. Estrogenicity is favored by bulky side chains and can be effectively abrogated by an (additional) linear substituent. Compound 2g, which lacks estrogenicity while potently inhibiting STS, has an ideal in vitro profile for the treatment of breast cancer.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Nussbaumer P,Winiski AP,Billich A

doi

10.1021/jm030926s

keywords:

subject

Has Abstract

pub_date

2003-11-06 00:00:00

pages

5091-4

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

杂志文章

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