Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing

The present report describes development of a novel, bifunctional molecule possessing both selective antiproliferative activity and siRNA transfection ability. We synthesized a series of cationic lipo-benzamides and screened for in vitro anticancer activities against a panel of cancer and non-cancer...

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Veröffentlicht in:European journal of medicinal chemistry 2012-10, Vol.56, p.400-408
Hauptverfasser: Muktapuram, Prathap Reddy, Gara, Rishi Kumar, Sharma, Komal, Rohit, Chilappa, Srinivas, Kolupula, Mishra, Durga Prasad, Bathula, Surendar Reddy
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Sprache:eng
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Zusammenfassung:The present report describes development of a novel, bifunctional molecule possessing both selective antiproliferative activity and siRNA transfection ability. We synthesized a series of cationic lipo-benzamides and screened for in vitro anticancer activities against a panel of cancer and non-cancer cells. The molecule with a ten carbon chain-length (C10M) significantly inhibited proliferation of cancer cells via arresting the cell cycle predominantly in the G1 phase; but did not affect non-cancerous cells. C10M effectively mediated siRNA delivery in vitro. The combined anticancer effect of the delivery of C10M together with its survivin-targeting siRNA cargo was significantly (p 
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2012.07.035