Literature DB >> 27161804

Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors.

Mauro Di Matteo1, Alessandra Ammazzalorso1, Federico Andreoli2, Irene Caffa3, Barbara De Filippis1, Marialuigia Fantacuzzi1, Letizia Giampietro1, Cristina Maccallini1, Alessio Nencioni3, Marco Daniele Parenti4, Debora Soncini3, Alberto Del Rio5, Rosa Amoroso1.   

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.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anticancer agents; Aromatase inhibitor; Imidazole; Sulfonamide; Synthesis

Mesh:

Substances:

Year:  2016        PMID: 27161804     DOI: 10.1016/j.bmcl.2016.04.078

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  New Oxazolo[5,4-d]pyrimidines as Potential Anticancer Agents: Their Design, Synthesis, and In Vitro Biological Activity Research.

Authors:  Aleksandra Sochacka-Ćwikła; Marcin Mączyński; Żaneta Czyżnikowska; Benita Wiatrak; Izabela Jęśkowiak; Albert Czerski; Andrzej Regiec
Journal:  Int J Mol Sci       Date:  2022-10-02       Impact factor: 6.208

2.  Towards an Understanding of the Mode of Action of Human Aromatase Activity for Azoles through Quantum Chemical Descriptors-Based Regression and Structure Activity Relationship Modeling Analysis.

Authors:  Chayawan Chayawan; Cosimo Toma; Emilio Benfenati; Ana Y Caballero Alfonso
Journal:  Molecules       Date:  2020-02-08       Impact factor: 4.411

  2 in total

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