Estrogenic Potential of 2-Alkyl-4-(thio)chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase
- 23 September 2003
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 46 (23) , 5091-5094
- https://doi.org/10.1021/jm030926s
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.Keywords
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