Pharmacophore Hybridization to Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity

Abstract

We used a pharmacophore hybridization strategy to combine key structural elements of merbarone and etoposide and generated new type II topoisomerase (topoII) poisons. This first set of hybrid topoII poisons shows promising antiproliferative activity on human cancer cells, endorsing their further exploration for anticancer drug discovery.