preparation of 16β-estradiol derivative libraries as bisubstrate inhibitors of 17β-hydroxysteroid dehydrogenase type 1 using the multidetachable sulfamate linker准备16β-estradiol导数库bisubstrate 17β-hydroxysteroid脱氢酶抑制剂1型使用multidetachable氨基磺酸盐链接器.pdfVIP

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preparation of 16β-estradiol derivative libraries as bisubstrate inhibitors of 17β-hydroxysteroid dehydrogenase type 1 using the multidetachable sulfamate linker准备16β-estradiol导数库bisubstrate 17β-hydroxysteroid脱氢酶抑制剂1型使用multidetachable氨基磺酸盐链接器.pdf

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preparation of 16β-estradiol derivative libraries as bisubstrate inhibitors of 17β-hydroxysteroid dehydrogenase type 1 using the multidetachable sulfamate linker准备16β-estradiol导数库bisubstrate 17β-hydroxysteroid脱氢酶抑制剂1型使用multidetachable氨基磺酸盐链接器

Molecules 2010, 15, 1590-1631; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420–3049 /journal/molecules Article Preparation of 16β-Estradiol Derivative Libraries as Bisubstrate Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 Using the Multidetachable Sulfamate Linker Marie Bérubé, Florian Delagoutte and Donald Poirier * Laboratory of Medicinal Chemistry, CHUQ (CHUL), Research Center and Laval University, Quebec, G1V 4G2, Canada * Author to whom correspondence should be addressed; E-Mail: donald.poirier@crchul.ulaval.ca. Received: 26 January 2010; in revised form: 8 February 2010 / Accepted: 3 March 2010 / Published: 10 March 2010 Abstract: Combinatorial chemistry is a powerful tool used to rapidly generate a large number of potentially biologically active compounds. In our goal to develop bisubstrate inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) that interact with both the substrate (estrone or estradiol) and the cofactor (NAD(P)H) binding sites, we used parallel solid-phase synthesis to prepare three libraries of 16β-estradiol derivatives with two or three levels of molecular diversity. From estrone, we first synthesized a sulfamate precursor that we loaded on trityl chloride resin using the efficient multidetachable sulfamate linker strategy recently developed in our laboratory. We then introduced molecular diversity [one or two amino acid(s) followed by a carboxylic acid] on s