Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents.
Authors of this article are:
Cincinelli R1, Musso L1, Artali R2, Guglielmi MB3, La Porta I3, Melito C3, Colelli F3, Cardile F3, Signorino G3, Fucci A3, Frusciante M3, Pisano C3, Dallavalle S1.
A summary of the article is shown below:
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.
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