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Design and synthesis of new inhibitors of p53–MDM2 interaction with a chalcone ...
Pereira, D; Lima, RT; Palmeira, A; Seca, H; Soares, J; Gomes, S; Raimundo, L; Maciel, C; Pinto, M; Sousa, E; Vasconcelos, MH; Saraiva, L; Cidade, HThe virtual screening of a library of chalcone derivatives led us to the identification of potential new MDM2 ligands. The chalcones with the best docking scores obeying the Lipinski rule of five were subsequently prepared by base-catalyzed aldol reactions. The activity of these compounds as inhibitors of p53–MDM2 interaction was investigated using a yeast-based screening assay. Using this approach two chalcone...
Date: 2019
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Origin: Repositório Aberto da Universidade do Porto