862269-71-4Relevant academic research and scientific papers
Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors
Cincinelli, Raffaella,Musso, Loana,Artali, Roberto,Guglielmi, Mario,Bianchino, Erminia,Cardile, Francesco,Colelli, Fabiana,Pisano, Claudio,Dallavalle, Sabrina
, p. 2005 - 2014 (2018)
Recent studies have demonstrated enhanced anticancer effects of combination therapy consisting of camptothecin derivatives and HDAC inhibitors. To exploit this synergy in a single active compound, we designed new dual-acting multivalent molecules simultaneously targeting topoisomerase I and HDAC. In particular, a selected compound containing a camptothecin and the psammaplin A scaffold 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.
