| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1397434 | European Journal of Medicinal Chemistry | 2012 | 9 Pages |
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 < 0.05) superior to that of agent alone. To our knowledge, this is the first report of a dual-purpose molecule with intrinsic anticancer activity and suitability for use in siRNA delivery.
Graphical abstractA novel cationic lipo-benzamide that not only selectively induce apoptosis in prostate cancer cells as compared to non-cancerous cells of prostate tissue in much the same way as targeted-anticancer agents but also self assembles and delivers siRNA.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Discovery of a molecule with anticancer activity and siRNA transfection ability. ► Novel benzamide derivatives were synthesized. ► Ten carbon lipobenzamide exhibit anticancer activity and siRNA transfection ability.
