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Title: Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2
Authors: Christodoulou, Michael S ×
Calogero, Francesco
Baumann, Marcus
García-Argáez, Aída Nelly
Pieraccini, Stefano
Sironi, Maurizio
Dapiaggi, Federico
Bucci, Raffaella
Broggini, Gianluigi
Gazzola, Silvia
Liekens, Sandra
Silvani, Alessandra
Lahtela-Kakkonen, Maija
Martinet, Nadine
Nonell-Canals, Alfons
Santamaría-Navarro, Eduardo
Baxendale, Ian R
Dalla Via, Lisa
Passarella, Daniele #
Issue Date: Mar-2015
Series Title: European Journal of Medicinal Chemistry vol:92 pages:766-775
Article number: S0223-5234(15)00058-6
Abstract: Two synthetic approaches to boehmeriasin A are described. A gram scale racemic preparation is accompanied by an efficient preparation of both the pure enantiomers using the conformationally stable 2-piperidin-2-yl acetaldehyde as starting material. The anti-proliferative activity in three cancer cell lines (CEM, HeLa and L1210) and two endothelial cell lines (HMEC-1, BAEC) indicates promising activity at the nanomolar range. Topoisomerases and SIRT2 are identified as biological targets and the experimental data has been supported by docking studies.
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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