Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
Eur J Med Chem
; 92: 766-75, 2015 Mar 06.
Article
em En
| MEDLINE
| ID: mdl-25626146
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.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Fenantrenos
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Quinolizidinas
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Sirtuína 2
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Inibidores da Topoisomerase I
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Inibidores da Topoisomerase II
Limite:
Humans
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article