SYNTHESIS OF N-omega-PHENYLALKYL-4-(p-CHLOROPHENYL)-PIPERIDIN-4-OL ANALOGUES WITH POTENT ANTIPROLIFERATIVE ACTIVITY AGAINST HCT-116 CELLS

摘要

Some opioid analogues, such as morphine and loperamide, were reported to exhibit weak antiproliferative activity against tumor cells. In a study of loperamide analogues, we found that adding an N-omega-phenylalkyl group onto the 4-arylpiperidin-4-ol unit can have important effects on the antiproliferative activity of such compounds against HCT-116 cells. We optimized the distance between the phenyl group and 4-arylpiperidin unit to promote such activity.