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

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. (C) 2016 Elsevier Ltd. All rights reserved.