LAUSR

A facile one-pot synthesis of new pyrimido[1,6-a]thieno[2,3-d]pyrimidin-4-ones , is reported via base-catalyzed reaction of 2-amino-3-cyanothiophenes , with 2,4-dichloro-5-bromo-6-methylpyrimidine . Subsequent treatment of the products with several amines under a mild condition gave a host of the new amino derivatives . The target compounds were evaluated for antiproliferative activity by an 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium assay on human breast cancer (MCF-7) and mouse fibroblast nonmalignant (L929) cell lines. The activation was structural, concentration, and time dependent. Doses inducing 50% cell-growth inhibition (IC50) for compounds , and against MCF-7 cells were explored. Compounds and as the two most potent analogs induced a sub-G1 peak in the flow-cytometry histogram of treated cells, compared with control, indicating that apoptotic cell death is involved in compound -induced and compound -induced toxicity. Compounds and exerted cytotoxic and proapototic effects on MCF-7 cell line.