American Chemical Society
jm7b01388_si_002.csv (12.82 kB)

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

Download (12.82 kB)
Version 2 2017-11-10, 17:04
Version 1 2017-11-09, 19:37
posted on 2017-10-27, 00:00 authored by Jose Antonio Ortega, Laura Riccardi, Elirosa Minniti, Marco Borgogno, Jose M. Arencibia, Maria L. Greco, Anna Minarini, Claudia Sissi, Marco De Vivo
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.