Efficient Synthesis of New Thieno[2,3-d]pyrimidin-4(3H)-one Derivatives for Evaluation as Anticancer Agents

Thieno[2,3-d]pyrimidinones were reported to act as potent anticancer agents; in this work, a series of new substituted thieno[2,3-d]pyrimidinone (6) were synthesized via the aza-Wittig reaction in satisfactory yields. The structures of these compounds were confirmed by elemental analysis, IR, 1H-NMR, and mass spectral data, and compound 6h was further analyzed by single crystal X-ray diffraction. Cytotoxic effect of all the compounds was carried out on human breast and lung cancer cell lines (MCF-7 and SPC-A-1, A459). Compound 6f exhibited the best inhibition activities against A459 with IC50 4.1M.