Synthesis and Cytotoxic Activity of Novel 9-[Hydroxy(Substitutedphenyl) Methyl]-2,2- Dimethyl-2,3,8,9-Tetrahydro-4H,10H-Pyrano [2,3-f ]Chromene-4,10-Diones

Chromanone derivatives demonstrate remarkable cytotoxity against a varieties of cancer cell lines. novel 9-[hydroxy(substitutedphenyl)methyl]-2,2-dimethyl-2,3,8,9- tetrahydro- 4h,10h-pyrano[2,3-f]chromene-4,10-diones as glyasperin analogues were synthesized in four steps from known 4-chromone 1. the key step was the preparation of chromane dione 5a by regioselective intramolecular cyclization reaction in 85% yield. condensation of 5a with substituted aromatic aldehydes afforded corresponding alpha hydroxybenzyl analogues 6a-6e. the cytotoxic study of the synthesized compounds against breast cancer human cell line (t47d) showed moderate cytotoxic activities (ic50=16-40 μm) compared to the positive control drug vincristin (ic50=2.5 μm).