Design, Synthesis and Anticancer Activity of a New Series of N-aryl-N′-[4-(pyridin-2-ylmethoxy)benzyl]urea Derivatives

The development of cancer treatments requires continuous exploration and improvement, in which the discovery of new drugs for the treatment of cancer is still an important pathway. In this study, based on the molecular hybridization strategy, a new structural framework with an N-aryl-N'-arylmethylurea scaffold was designed, and 16 new target compounds were synthesized and evaluated for their antiproliferative activities against four different cancer cell lines A549, MCF7, HCT116, PC3, and human liver normal cell line HL7702. The results have shown seven compounds with 1-methylpiperidin-4-yl groups having excellent activities against all four cancer cell lines, and they exhibited scarcely any activities against HL7702. Among them, compound 9b and 9d showed greatly excellent activity against the four kinds of cells, and the IC50 for MCF7 and PC3 cell lines were even less than 3 mu M.

Automated summary

The study designed a new structural framework for anti-cancer compounds using molecular hybridization strategy, and synthesized 16 new target compounds. Seven compounds were found to exhibit excellent antiproliferative activities against four different cancer cell lines, with minimal activities against normal cell lines. Compound 9b and 9d showed particularly outstanding activity against all four cancer cell lines, with IC50 values less than 3 micromolar for MCF7 and PC3 cell lines.