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ID: ALA3407358

Journal: Eur J Med Chem

Title: Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.

Authors: Christodoulou MS, Calogero F, Baumann M, García-Argáez AN, Pieraccini S, Sironi M, Dapiaggi F, Bucci R, Broggini G, Gazzola S, Liekens S, Silvani A, Lahtela-Kakkonen M, Martinet N, Nonell-Canals A, Santamaría-Navarro E, Baxendale IR, Dalla Via L, Passarella D.

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.

CiteXplore: 25626146

DOI: 10.1016/j.ejmech.2015.01.038