Abstract A novel domino intramolecular [3+2] cycloaddtion and ring-opening aromatization process has been successfully developed for the efficient direct synthesis of pyrrolyl or indolyl substituted 9,10-dihydrophenanthren-9-ol analogues. And 1-(phenanthren-9-yl)-1H-pyrroles can… Click to show full abstract
Abstract A novel domino intramolecular [3+2] cycloaddtion and ring-opening aromatization process has been successfully developed for the efficient direct synthesis of pyrrolyl or indolyl substituted 9,10-dihydrophenanthren-9-ol analogues. And 1-(phenanthren-9-yl)-1H-pyrroles can be easily obtained via dehydration of 10-(1H-pyrrol-1-yl)-9,10-dihydrophenanthren-9-ols. Furthermore, the MTT assay indicated that four compounds with indolyl substitutions showed obvious inhibitory activities against HepG2 cells, and compound anti-4jb displayed a lowest IC50 value of 9.99 μM.
Journal Title: Tetrahedron Letters
Year Published: 2020
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