Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents.
basic_science · Level V
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- Record sourced from PubMed, PMID 30300374.
- Also identified by DOI 10.1371/journal.pone.0205018 and PMC identifier 6177136.
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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.
Medical subject headings
- Antineoplastic Agents
- Histone Deacetylase Inhibitors
- Neoplasms
- Topoisomerase I Inhibitors