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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Development of novel steroid sulfatase inhibitors. I. Synthesis and biological evaluation of biphenyl-4-O-sulfamates.

Compounds which interfere with steroid sulfatase ( STS) are expected as important novel therapeutic drugs for postmenopausal breast tumor. Therefore, a number of strategies have been adopted to design and synthesize potent, nonestrogenic STS inhibitors. We chose biphenyl as a scaffold for STS inhibitors and synthesized some biphenyl-4-O-sulfamate derivatives (29-43). Their inhibitory activity on STS and estrogenicity were evaluated. Substitution of electron-withdrawing groups (e.g., cyano, nitro) at the 2'- or 4'-position of biphenyl-4-O-sulfamate remarkably increased STS-inhibitory activity. Especially, 2',4'-dicyanobiphenyl-4-O-sulfamate (35, TZS-8478) showed very potent STS-inhibitory activity in vitro. The administration of TZS-8478 (0.5 mg/kg per day, p.o., for 5 days) completely inhibited rat liver and uterine STS similarly to EMATE (1). Furthermore, TZS-8478 (10 mg/kg per day, p.o., for 5 days) had no stimulative effect on uterine growth in ovariectomized rats, and its desulfamoylated compound (20) was little bound to the human estrogen receptor alpha. The identification of a potent steroid sulfatase inhibitor without estrogenicity, such as TZS-8478, should be of considerable value in evaluating the potential of steroid sulfatase inhibition for breast tumor therapy.[1]

References

  1. Development of novel steroid sulfatase inhibitors. I. Synthesis and biological evaluation of biphenyl-4-O-sulfamates. Okada, M., Nakagawa, T., Iwashita, S., Takegawa, S., Fujii, T., Koizumi, N. J. Steroid Biochem. Mol. Biol. (2003) [Pubmed]
 
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