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ID: ALA1135104

Journal: Bioorg Med Chem Lett

Title: A novel type of nonsteroidal estrone sulfatase inhibitors.

Authors: Jütten P, Schumann W, Härtl A, Heinisch L, Gräfe U, Werner W, Ulbricht H.

Abstract: Madurahydroxylactone (MHL) is a secondary metabolite produced by the soil bacterium Nonomuria rubra and belongs to the family of benzo[a]naphthacenequinones. We report the initial results and structure-activity relationships of our study into a series of thiosemicarbazone derivatives of madurahydroxylactone as potential nonsteroidal inhibitors of the enzyme estrone sulfatase. The most active compound, the cyclohexylthiosemicarbazone, was shown to be a non-competitive inhibitor with a K(i) of 0.35microM. This compound is devoid of estrogenic properties and showed low acute toxicity in the hen's fertile egg screening test.

CiteXplore: 11992772

DOI: 10.1016/s0960-894x(02)00171-3