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 |
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| container_title | European journal of medicinal chemistry |
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| creator | Muktapuram, Prathap Reddy Gara, Rishi Kumar Sharma, Komal Rohit, Chilappa Srinivas, Kolupula Mishra, Durga Prasad Bathula, Surendar Reddy |
| description | 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 |
| doi_str_mv | 10.1016/j.ejmech.2012.07.035 |
| format | Article |
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[Display omitted] A 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.
► 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.</description><identifier>ISSN: 0223-5234</identifier><identifier>EISSN: 1768-3254</identifier><identifier>DOI: 10.1016/j.ejmech.2012.07.035</identifier><identifier>PMID: 22926227</identifier><identifier>CODEN: EJMCA5</identifier><language>eng</language><publisher>Kidlington: Elsevier Masson SAS</publisher><subject>Animals ; Anticancer molecule ; Anticancer siRNA ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Apoptosis - drug effects ; Benzamides - chemical synthesis ; Benzamides - chemistry ; Benzamides - pharmacology ; Biological and medical sciences ; Cell Line, Tumor ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; Cercopithecus aethiops ; Combination therapy ; COS Cells ; Dose-Response Relationship, Drug ; Drug Delivery Systems ; Drug Screening Assays, Antitumor ; Gene Silencing - drug effects ; Hep G2 Cells ; Humans ; MCF-7 Cells ; Medical sciences ; Mice ; Miscellaneous ; Models, Molecular ; Molecular Structure ; NIH 3T3 Cells ; Pharmacology. Drug treatments ; RNA, Small Interfering - genetics ; RNA, Small Interfering - metabolism ; RNA, Small Interfering - pharmacology ; Structure-Activity Relationship ; Survivin gene</subject><ispartof>European journal of medicinal chemistry, 2012-10, Vol.56, p.400-408</ispartof><rights>2012 Elsevier Masson SAS</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2012 Elsevier Masson SAS. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c392t-d70cc498163c29e2fb365013e0ef526f4b79a010373674a7d052c3a4155bc58e3</citedby><cites>FETCH-LOGICAL-c392t-d70cc498163c29e2fb365013e0ef526f4b79a010373674a7d052c3a4155bc58e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0223523412004618$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26589453$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22926227$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Muktapuram, Prathap Reddy</creatorcontrib><creatorcontrib>Gara, Rishi Kumar</creatorcontrib><creatorcontrib>Sharma, Komal</creatorcontrib><creatorcontrib>Rohit, Chilappa</creatorcontrib><creatorcontrib>Srinivas, Kolupula</creatorcontrib><creatorcontrib>Mishra, Durga Prasad</creatorcontrib><creatorcontrib>Bathula, Surendar Reddy</creatorcontrib><title>Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing</title><title>European journal of medicinal chemistry</title><addtitle>Eur J Med Chem</addtitle><description>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.
[Display omitted] A 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.
► 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.</description><subject>Animals</subject><subject>Anticancer molecule</subject><subject>Anticancer siRNA</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Apoptosis - drug effects</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>Cercopithecus aethiops</subject><subject>Combination therapy</subject><subject>COS Cells</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Delivery Systems</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Gene Silencing - drug effects</subject><subject>Hep G2 Cells</subject><subject>Humans</subject><subject>MCF-7 Cells</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Miscellaneous</subject><subject>Models, Molecular</subject><subject>Molecular Structure</subject><subject>NIH 3T3 Cells</subject><subject>Pharmacology. Drug treatments</subject><subject>RNA, Small Interfering - genetics</subject><subject>RNA, Small Interfering - metabolism</subject><subject>RNA, Small Interfering - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Survivin gene</subject><issn>0223-5234</issn><issn>1768-3254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1v1DAURS1ERaeFf4CQN0hsEp6_JyyQRhUUpKqVKlhbjvNSHJy42JlB8-_JaAa6Y_U25953dQh5zaBmwPT7ocZhRP-j5sB4DaYGoZ6RFTN6XQmu5HOyAs5FpbiQ5-SilAEAlAZ4Qc45b7jm3KzIsJnm4N3kMdMS7m83tMMYdpj3tN3TCX9T9wSMKaLfRvxAN3RKO4zUp7ENk5tDmmiZs5vxYU_7lOkp4TFG-jPEGKaHl-Ssd7Hgq9O9JN8_f_p29aW6ubv-erW5qbxo-Fx1BryXzZpp4XmDvG-FVsAEAvaK6162pnHAQBihjXSmA8W9cJIp1Xq1RnFJ3h17H3P6tcUy2zGUwxA3YdoWyxiTujFMwYLKI-pzKiVjbx9zGF3eWwb2YNkO9mjZHixbMHaxvMTenD5s2xG7f6G_Whfg7QlwxbvY58VGKE-cVutGKrFwH48cLj52AbMtPuBirgsZ_Wy7FP6_5A-yfpxF</recordid><startdate>20121001</startdate><enddate>20121001</enddate><creator>Muktapuram, Prathap Reddy</creator><creator>Gara, Rishi Kumar</creator><creator>Sharma, Komal</creator><creator>Rohit, Chilappa</creator><creator>Srinivas, Kolupula</creator><creator>Mishra, Durga Prasad</creator><creator>Bathula, Surendar Reddy</creator><general>Elsevier Masson SAS</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20121001</creationdate><title>Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing</title><author>Muktapuram, Prathap Reddy ; Gara, Rishi Kumar ; Sharma, Komal ; Rohit, Chilappa ; Srinivas, Kolupula ; Mishra, Durga Prasad ; Bathula, Surendar Reddy</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c392t-d70cc498163c29e2fb365013e0ef526f4b79a010373674a7d052c3a4155bc58e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Animals</topic><topic>Anticancer molecule</topic><topic>Anticancer siRNA</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Apoptosis - drug effects</topic><topic>Benzamides - chemical synthesis</topic><topic>Benzamides - chemistry</topic><topic>Benzamides - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation - drug effects</topic><topic>Cell Survival - drug effects</topic><topic>Cercopithecus aethiops</topic><topic>Combination therapy</topic><topic>COS Cells</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Delivery Systems</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Gene Silencing - drug effects</topic><topic>Hep G2 Cells</topic><topic>Humans</topic><topic>MCF-7 Cells</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Miscellaneous</topic><topic>Models, Molecular</topic><topic>Molecular Structure</topic><topic>NIH 3T3 Cells</topic><topic>Pharmacology. Drug treatments</topic><topic>RNA, Small Interfering - genetics</topic><topic>RNA, Small Interfering - metabolism</topic><topic>RNA, Small Interfering - pharmacology</topic><topic>Structure-Activity Relationship</topic><topic>Survivin gene</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Muktapuram, Prathap Reddy</creatorcontrib><creatorcontrib>Gara, Rishi Kumar</creatorcontrib><creatorcontrib>Sharma, Komal</creatorcontrib><creatorcontrib>Rohit, Chilappa</creatorcontrib><creatorcontrib>Srinivas, Kolupula</creatorcontrib><creatorcontrib>Mishra, Durga Prasad</creatorcontrib><creatorcontrib>Bathula, Surendar Reddy</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Muktapuram, Prathap Reddy</au><au>Gara, Rishi Kumar</au><au>Sharma, Komal</au><au>Rohit, Chilappa</au><au>Srinivas, Kolupula</au><au>Mishra, Durga Prasad</au><au>Bathula, Surendar Reddy</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing</atitle><jtitle>European journal of medicinal chemistry</jtitle><addtitle>Eur J Med Chem</addtitle><date>2012-10-01</date><risdate>2012</risdate><volume>56</volume><spage>400</spage><epage>408</epage><pages>400-408</pages><issn>0223-5234</issn><eissn>1768-3254</eissn><coden>EJMCA5</coden><abstract>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.
[Display omitted] A 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.
► 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.</abstract><cop>Kidlington</cop><pub>Elsevier Masson SAS</pub><pmid>22926227</pmid><doi>10.1016/j.ejmech.2012.07.035</doi><tpages>9</tpages></addata></record> |
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| identifier | ISSN: 0223-5234 |
| ispartof | European journal of medicinal chemistry, 2012-10, Vol.56, p.400-408 |
| issn | 0223-5234 1768-3254 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Anticancer molecule Anticancer siRNA Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis - drug effects Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Cercopithecus aethiops Combination therapy COS Cells Dose-Response Relationship, Drug Drug Delivery Systems Drug Screening Assays, Antitumor Gene Silencing - drug effects Hep G2 Cells Humans MCF-7 Cells Medical sciences Mice Miscellaneous Models, Molecular Molecular Structure NIH 3T3 Cells Pharmacology. Drug treatments RNA, Small Interfering - genetics RNA, Small Interfering - metabolism RNA, Small Interfering - pharmacology Structure-Activity Relationship Survivin gene |
| title | Anticancer siRNA delivery by new anticancer molecule: A novel combination strategy for cancer cell killing |
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