4, 4′-Benzophenone-O, O′-disulfamate: a potent inhibitor of steroid sulfatase

P Nussbaumer, M Bilban, A Billich

Index: Nussbaumer, Peter; Bilban, Melitta; Billich, Andreas Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 16 p. 2093 - 2095

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Citation Number: 29

Abstract

We investigated whether the benzophenone moiety can be used as core element of steroid sulfatase (STS) inhibitors. While 4-and 3-benzophenone-O-sulfamates inhibit STS with IC50 values between 5 and 7μM irrespective of additional hydroxy and methoxy substituents at the second phenyl ring, benzophenone-O, O′-disulfamates show increased activity. With an IC50 value of 190nM the 4, 4′-derivative is the first small monocyclic STS inhibitor ...