2. Academic Validation
  3. Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity

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

  • J Med Chem. 2018 Feb 8;61(3):1375-1379. doi: 10.1021/acs.jmedchem.7b01388.
Jose Antonio Ortega 1,  Laura Riccardi 1,  Elirosa Minniti 1 2,  Marco Borgogno 1,  Jose M Arencibia 1,  Maria L Greco 3,  Anna Minarini 2,  Claudia Sissi 3,  Marco De Vivo 1 4
Affiliations

Affiliations

  • 1 Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia , Via Morego 30, 16163 Genova, Italy.
  • 2 Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna , Via Belmeloro 6, 40126 Bologna, Italy.
  • 3 Department of Pharmaceutical and Pharmacological Sciences, University of Padova , Via Marzolo 5, 35131 Padova, Italy.
  • 4 IAS-5/INM-9 Computational Biomedicine Forschungszentrum Jülich , Wilhelm-Johnen-Straße, 52428 Jülich, Germany.
PMID: 29077404 DOI: 10.1021/acs.jmedchem.7b01388
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.

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