Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2- d ]pyrimidin-4-amine Analogs of MPC-6827.

Efficient microwave-assisted chemical processes were applied to the synthesis of an array of novelN-(4-methoxyphenylamino)-2-methyl benzo-, pyrido- or pyrazino-thieno[3,2-d]pyrimidin-4-amine derivatives. These heteroaromatic systems were envisioned as potent bioisosteric analogues ofMPC-6827, an anticancer agent previously developed until phase II clinical studies. A brief evaluation and comparison of their antiproliferative activity on HT-29 and Caco-2, two human colorectal cancer cell lines, were also reported. At the tested concentrations (5 and 10 mu M), thieno[3,2-d]pyrimidin-4-amines4aand4cexhibited an inhibitory effect similar toMPC-6827on human colorectal cancer cell proliferation.