Data di Pubblicazione:
2015
Citazione:
Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2 / M.S. Christodoulou, F. Calogero, M. Baumann, A.N. García-Argáez, S. Pieraccini, M. Sironi, F. Dapiaggi, R. Bucci, G. Broggini, S. Gazzola, S. Liekens, A. Silvani, M. Lahtela-Kakkonen, N. Martinet, A. Nonell-Canals, E. Santamaría-Navarro, I.R. Baxendale, L. Dalla Via, D. Passarella. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 92(2015 Mar 06), pp. 766-775.
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.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Boehmeriasin A Total synthesis; Sirtuins inhibition; Topoisomerases inhibition; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; Pharmacology
Elenco autori:
M.S. Christodoulou, F. Calogero, M. Baumann, A.N. García-Argáez, S. Pieraccini, M. Sironi, F. Dapiaggi, R. Bucci, G. Broggini, S. Gazzola, S. Liekens, A. Silvani, M. Lahtela-Kakkonen, N. Martinet, A. Nonell-Canals, E. Santamaría-Navarro, I.R. Baxendale, L. Dalla Via, D. Passarella
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