| Literature DB >> 25626146 |
Michael S Christodoulou1, Francesco Calogero1, Marcus Baumann2, Aída Nelly García-Argáez3, Stefano Pieraccini1, Maurizio Sironi1, Federico Dapiaggi1, Raffaella Bucci1, Gianluigi Broggini4, Silvia Gazzola4, Sandra Liekens5, Alessandra Silvani1, Maija Lahtela-Kakkonen6, Nadine Martinet7, Alfons Nonell-Canals8, Eduardo Santamaría-Navarro8, Ian R Baxendale2, Lisa Dalla Via3, Daniele Passarella9.
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.Entities:
Keywords: Boehmeriasin A; Sirtuins inhibition; Topoisomerases inhibition; Total synthesis
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Year: 2015 PMID： 25626146 DOI： 10.1016/j.ejmech.2015.01.038
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514