Yangmei Li

Urea and thiohydantoin are among the important privileged structures for drug discovery. We have developed a synthetic approach to the high‐throughput synthesis of the heterobivalent compounds containing both urea and 5‐arylidene‐2‐thiohydantoin functional groups. This synthetic methodology was applied to the synthesis of a mixture‐based library containing a total of 5280 compounds in a positional scanning format. The library was screened for its antiproliferative activity against cancer cells using a tetrazolium dye (MTT) based assay. Deconvolution of the library identified six hit compounds exhibiting moderate inhibitory potency against cancer cell proliferation.