Published 2016 | Version v1
Publication Metadata-only

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

Di Matteo M.
Ammazzalorso A.
Andreoli F.
Caffa I.
De Filippis B.
Fantacuzzi M.
Giampietro L.
Maccallini C.
Nencioni A.
Parenti M. D.
Soncini D.
Del Rio A.
Amoroso R.
Others:
Di Matteo, M.
Ammazzalorso, A.
Andreoli, F.
Caffa, I.
De Filippis, B.
Fantacuzzi, M.
Giampietro, L.
Maccallini, C.
Nencioni, A.
Parenti, M. D.
Soncini, D.
Del Rio, A.
Amoroso, R.

Description

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.

Additional details

Identifiers Origin repository
Created:
April 14, 2023
Modified:
November 30, 2023