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An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512.
Palermo G, Minniti E, Greco ML, Riccardi L, Simoni E, Convertino M, Marchetti C, Rosini M, Sissi C, Minarini A, De Vivo M. Palermo G, et al. Among authors: minniti e. Chem Commun (Camb). 2015 Oct 1;51(76):14310-3. doi: 10.1039/c5cc05065k. Epub 2015 Aug 3. Chem Commun (Camb). 2015. PMID: 26234198
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.
Ortega JA, Arencibia JM, Minniti E, Byl JAW, Franco-Ulloa S, Borgogno M, Genna V, Summa M, Bertozzi SM, Bertorelli R, Armirotti A, Minarini A, Sissi C, Osheroff N, De Vivo M. Ortega JA, et al. Among authors: minniti e. J Med Chem. 2020 Nov 12;63(21):12873-12886. doi: 10.1021/acs.jmedchem.0c00774. Epub 2020 Oct 20. J Med Chem. 2020. PMID: 33079544 Free PMC article.