Iodine catalyzed simple and efficient synthesis of antiproliferative 2-pyridones.

摘要: A simple and efficient method for the selective synthesis of 2-pyrdones from 4H-pyrans using iodine as catalyst ethanol solvent was developed. The present is equally effective both aromatic hetero ring containing 4H-pyrans. compatibility with various functional groups, mild reaction conditions, high yields application inexpensive, readily easily available formation 2-pyridones major products are advantages procedure. In vitro antiproliferative activity final synthesized compounds evaluated four different human cancer cell lines (Lung adenocarcinoma-A549, Hepatocarcinoma-HepG2, Breast carcinoma-MCF-7 Ovarian carcinoma-SKOV3) normal lung fibroblast line (MRC-5). Compounds 2b showed better inhibition against MCF-7, HepG2 A549 (IC50 8.00 ± 0.11, 11.93 0.01 15.85 0.04 μM, respectively) compared doxorubicin also 2e moderate 9.32 0.21 20.22 respectively, lines, doxorubicin. As many clinically used agents induce apoptosis in cells hence, 2-pyridone analogues were tested their ability to MCF-7 caspases-3 -9 assays.