Open AccessPharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Author(s) -
José Antonio Ortega,
Laura Riccardi,
Elirosa Minniti,
Marco Borgogno,
José M. Arencibia,
Maria Laura Greco,
Anna Minarini,
Claudia Sissi,
Marco De Vivo
Publication year - 2017
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/acs.jmedchem.7b01388
Subject(s) - pharmacophore , topoisomerase , chemistry , etoposide , topoisomerase inhibitor , drug discovery , computational biology , combinatorial chemistry , biochemistry , enzyme , genetics , biology , chemotherapy
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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