Estrogenic Potential of 2-Alkyl-4-(Thio)Chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase
September 2003
in “
Journal of Medicinal Chemistry
”
TLDR A substance called Compound 2g can strongly block STS (a hormone-related enzyme) without affecting estrogen levels, making it potentially good for treating breast cancer.
In 2003, a study was conducted on a new class of steroid sulfatase (STS) inhibitors, 2-Alkylchromen-4-one 6-O-sulfamates, to assess their estrogenic potential. The research found no correlation between estrogenic activity and STS inhibition. It was discovered that bulky side chains favor estrogenicity, which can be effectively eliminated by an additional linear substituent. Compound 2g, which inhibits STS powerfully without estrogenicity, was identified as having an ideal in vitro profile for breast cancer treatment.
