Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors. Issue 13 (1st July 2016)

• Record Type: Journal Article
• Authors: Di Matteo, Mauro; Ammazzalorso, Alessandra; Andreoli, Federico; Caffa, Irene; De Filippis, Barbara; Fantacuzzi, Marialuigia; Giampietro, Letizia; Maccallini, Cristina; Nencioni, Alessio; Parenti, Marco Daniele; Soncini, Debora; Del Rio, Alberto; Amoroso, Rosa
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 13(2016)
• Page Start: 3192
• Page End: 3194
• Publication Date: 2016-07-01
• Subjects: Aromatase inhibitor -- Imidazole -- Anticancer agents -- Synthesis -- Sulfonamide; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.04.078
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The most frequently used treatment for hormone receptor positive breast cancer in post-menopausal women are aromatase inhibitors. In order to develop new aromatase inhibitors, we designed and synthesized new imidazolylmethylpiperidine sulfonamides using the structure of the previously identified aromatase inhibitor SYN 20028567 as starting lead. By this approach, three new aromatase inhibitors with IC50 values that are similar to that of letrozole and SYN 20028567 were identified.