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2005
Steroids
U 0300
03- 182
Estrone Formate: A Novel Type of Irreversible Inhibitor of Human Steroid Sulfatase. — Estrone conjugates, substituted at C-3 of the steroid skeleton with different
functionalities are prepared. The synthesized estrone analogues are all inactive with exception of formate (I). Formate (I) inhibits steroid sulfatase in a time- and concentration-dependent manner and is the first potent inactivator of steroid sulfatase which does
not feature the sulfamate group. Surprisingly, the structurally quite different aryl formate (II) causes inactivation of the enzyme suggesting a general principle of inactivation by the formate group. An immediate transfer of the formyl group to a nucleophile
in the active site of steroid sulfatase is considered as a potential mode of action. —
(SCHREINER*, E. P.; BILLICH, A.; Bioorg. Med. Chem. Lett. 14 (2004) 19,
4999-5002; Novartis Inst. Biomed. Res., A-1235 Wien, Austria; Eng.) —
H. Hoennerscheid
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