TY - JOUR
T1 - Synthesis and biological characterization of 3-(imidazol-1-ylmethyl)piperidine sulfonamides as aromatase inhibitors
AU - Di Matteo, Mauro
AU - Ammazzalorso, Alessandra
AU - Andreoli, Federico
AU - Caffa, Irene
AU - De Filippis, Barbara
AU - Fantacuzzi, Marialuigia
AU - Giampietro, Letizia
AU - Maccallini, Cristina
AU - Nencioni, Alessio
AU - Parenti, Marco
AU - Soncini, Debora
AU - Del Rio, Alberto
AU - Amoroso, Rosa
PY - 2016/3/17
Y1 - 2016/3/17
N2 - 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.
AB - 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.
KW - Anticancer agents
KW - Aromatase inhibitor
KW - Imidazole
KW - Sulfonamide
KW - Synthesis
UR - http://www.scopus.com/inward/record.url?scp=84965020612&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84965020612&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2016.04.078
DO - 10.1016/j.bmcl.2016.04.078
M3 - Article
AN - SCOPUS:84965020612
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
ER -