Synthesis and antiproliferative activity of 2,4-disubstituted 6-aryl-7 H-pyrrolo[3,2- d]pyrimidin-7-one 5-oxides

Abstract

A series of 2,4-disubstituted 6-aryl-7 H-pyrrolo[3,2- d]pyrimidin-7-one 5-oxides were synthesized and in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, HBL-100, HeLa, SW1573, T-47D, and WiDr. The most potent analog induced considerably growth inhibition in the range 0.35–2.0 μM. Cell cycle studies in the breast and lung cancer cells revealed arrest in the G 2/M compartment. The results showed that the title compounds bearing alkylamino or dialkylamino moieties in position 2 of the pyrimidine ring are more active than those bearing hydrogen or methylthio groups.