SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL DISPIRO COMPOUNDS BASED ON 5-ARYLIDENEHYDANTOINS AND ISATINS AS INHIBITORS OF P53–MDM2 PROTEIN–PROTEIN INTERACTION
DOI:
https://doi.org/10.1007/5613Ключевые слова:
hydantoins, spirooxindole, anticancer drugs, 1, 3-dipolar cycloaddition, p53–MDM2 inhibitors.Аннотация
A series of novel hydantoin-based dispiroindolinones as potential small-molecule inhibitors of p53–MDM2 protein–protein interaction were synthesized by two methods, using 2-arylidenehydantoins as starting materials. Some compounds demonstrate moderate cytotoxicity against cancer cell lines with IC50 in micromolar concentration range, which is comparable to nutlin-3. Two of the synthesized dispiroindolinones show p53-related activity in p53 reporter activation test.
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Опубликован
2020-07-10
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Оригинальные статьи