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.
Ortega, J.A., Riccardi, L., Minniti, E., Borgogno, M., Arencibia, J.M., Greco, M.L., et al. (2018). Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity. JOURNAL OF MEDICINAL CHEMISTRY, 61(3), 1375-1379 [10.1021/acs.jmedchem.7b01388].
Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Minniti, Elirosa;Borgogno, Marco;Minarini, Anna;
2018
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.| File | Dimensione | Formato | |
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