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- Title
Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents.
- Authors
Cincinelli, Raffaella; Musso, Loana; Artali, Roberto; Guglielmi, Mario B.; La Porta, Ilaria; Melito, Carmela; Colelli, Fabiana; Cardile, Francesco; Signorino, Giacomo; Fucci, Alessandra; Frusciante, Martina; Pisano, Claudio; Dallavalle, Sabrina
- Abstract
Recent studies have shown that HDAC inhibitors act synergistically with camptothecin derivatives in combination therapies. To exploit this synergy, new hybrid molecules targeting simultaneously topoisomerase I and HDAC were designed. In particular, a selected multivalent agent containing a camptothecin and a SAHA-like template showed a broad spectrum of antiproliferative activity, with IC50 values in the nanomolar range. Preliminary in vivo results indicated a strong antitumor activity on human mesothelioma primary cell line MM473 orthotopically xenografted in CD-1 nude mice and very high tolerability.
- Subjects
DNA topoisomerase I; ANTINEOPLASTIC agents; CAMPTOTHECIN; XENOGRAFTS; PHYSICAL &; theoretical chemistry
- Publication
PLoS ONE, 2018, Vol 13, Issue 10, p1
- ISSN
1932-6203
- Publication type
Article
- DOI
10.1371/journal.pone.0205018