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

Efficient microwave-assisted chemical processes were applied to the synthesis of an array of novel -(4-methoxyphenylamino)-2-methyl benzo-, pyrido- or pyrazino-thieno[3,2-]pyrimidin-4-amine derivatives. These heteroaromatic systems were envisioned as potent bioisosteric analogues of , 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 µM), thieno[3,2-]pyrimidin-4-amines and exhibited an inhibitory effect similar to on human colorectal cancer cell proliferation.