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

Bioorganic & Medicinal Chemistry Letters
2016.0

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.

Knowledge Graph

Similar Paper

Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors
Bioorganic & Medicinal Chemistry Letters 2016.0
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series
Bioorganic & Medicinal Chemistry Letters 2012.0
Synthesis of some imidazolyl-substituted 2-benzylidene indanone derivatives as potent aromatase inhibitors for breast cancer therapy
Medicinal Chemistry Research 2011.0
Synthesis of imidazole-derived steroidal hybrids as potent aromatase inhibitors
Medicinal Chemistry Research 2013.0
Preparation and pharmacological profile of 7-(α-Azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: Potent and selective aromatase inhibitors
Bioorganic & Medicinal Chemistry Letters 2006.0
Design, Synthesis, and Biological Evaluation of Imidazolyl Derivatives of 4,7-Disubstituted Coumarins as Aromatase Inhibitors Selective over 17-α-Hydroxylase/C17−20 Lyase
Journal of Medicinal Chemistry 2011.0
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity
Bioorganic & Medicinal Chemistry Letters 2017.0
Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors
European Journal of Medicinal Chemistry 2020.0
Synthesis, structure-activity relationships and molecular docking studies of phenyldiazenyl sulfonamides as aromatase inhibitors
European Journal of Medicinal Chemistry 2021.0