Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs
Acyl derivatives of boswellic acids including their epimers were synthesized and screened against a panel of cancer cell lines. One of the lead compounds was found to be an inhibitor of NF-κB and STAT proteins. Boswellic acid acylates including their epimers were synthesized and screened against a p...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2012-01, Vol.22 (1), p.431-435 |
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| container_end_page | 435 |
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| container_issue | 1 |
| container_start_page | 431 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 22 |
| creator | Kumar, Ajay Shah, Bhahwal A. Singh, Samar Hamid, Abid Singh, Shashank K. Sethi, Vijay K. Saxena, Ajit K. Singh, Jaswant Taneja, Subhash C. |
| description | Acyl derivatives of boswellic acids including their epimers were synthesized and screened against a panel of cancer cell lines. One of the lead compounds was found to be an inhibitor of NF-κB and STAT proteins.
Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead. |
| doi_str_mv | 10.1016/j.bmcl.2011.10.112 |
| format | Article |
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Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2011.10.112</identifier><identifier>PMID: 22123322</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Acyl derivatives ; Anti-cancer ; Antineoplastic Agents - pharmacology ; Biological and medical sciences ; Boswellic acids ; Cell Line, Tumor ; Cell Proliferation ; Drug Design ; Drug Screening Assays, Antitumor - methods ; Flow Cytometry - methods ; HL-60 Cells ; Humans ; Medical sciences ; Models, Chemical ; NF-kappa B - metabolism ; NF-κB ; Pharmacology. Drug treatments ; Phosphorylation ; STAT ; STAT Transcription Factors - metabolism ; Triterpenes - chemistry ; Triterpenes - pharmacology</subject><ispartof>Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.431-435</ispartof><rights>2011 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c385t-48c7c37fc75123e60f1624f1e9e8a73ddfd58114e4cb211252b86bf092bc1ada3</citedby><cites>FETCH-LOGICAL-c385t-48c7c37fc75123e60f1624f1e9e8a73ddfd58114e4cb211252b86bf092bc1ada3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X11015198$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,4010,27900,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=25413343$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22123322$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumar, Ajay</creatorcontrib><creatorcontrib>Shah, Bhahwal A.</creatorcontrib><creatorcontrib>Singh, Samar</creatorcontrib><creatorcontrib>Hamid, Abid</creatorcontrib><creatorcontrib>Singh, Shashank K.</creatorcontrib><creatorcontrib>Sethi, Vijay K.</creatorcontrib><creatorcontrib>Saxena, Ajit K.</creatorcontrib><creatorcontrib>Singh, Jaswant</creatorcontrib><creatorcontrib>Taneja, Subhash C.</creatorcontrib><title>Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Acyl derivatives of boswellic acids including their epimers were synthesized and screened against a panel of cancer cell lines. One of the lead compounds was found to be an inhibitor of NF-κB and STAT proteins.
Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead.</description><subject>Acyl derivatives</subject><subject>Anti-cancer</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Boswellic acids</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation</subject><subject>Drug Design</subject><subject>Drug Screening Assays, Antitumor - methods</subject><subject>Flow Cytometry - methods</subject><subject>HL-60 Cells</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Models, Chemical</subject><subject>NF-kappa B - metabolism</subject><subject>NF-κB</subject><subject>Pharmacology. Drug treatments</subject><subject>Phosphorylation</subject><subject>STAT</subject><subject>STAT Transcription Factors - metabolism</subject><subject>Triterpenes - chemistry</subject><subject>Triterpenes - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtKAzEUhoMoWqsv4EJmI66m5jY3cFPFG4gurOAuZE5OMGU6o8m04qv5ED6Tqa26c3Xg8OU_fz5CDhgdMcryk-monkEz4pSx0XLH-AYZMJnLVEiabZIBrXKalpV82iG7IUwpZZJKuU12OGdcCM4H5GIM701i0LuF7t0CQ9LZpO7CGzaNg0SDMyHRIXHts6td3_lv4O4y_fw4S3RrkofJeBL2yJbVTcD99RySx8uLyfl1ent_dXM-vk1BlFmfyhIKEIWFIov3MaeW5VxahhWWuhDGWJOVjEmUUPP4nYzXZV5bWvEamDZaDMnxKvfFd69zDL2auQCxqm6xmwdVMSFiJC8iyVck-C4Ej1a9eDfT_l0xqpb21FQt7amlve9dbDQkh-v4eT1D8_vkR1cEjtaADqAb63ULLvxxmYwFpIjc6YrDKGPh0KsADltA4zxCr0zn_uvxBb9tjF8</recordid><startdate>20120101</startdate><enddate>20120101</enddate><creator>Kumar, Ajay</creator><creator>Shah, Bhahwal A.</creator><creator>Singh, Samar</creator><creator>Hamid, Abid</creator><creator>Singh, Shashank K.</creator><creator>Sethi, Vijay K.</creator><creator>Saxena, Ajit K.</creator><creator>Singh, Jaswant</creator><creator>Taneja, Subhash C.</creator><general>Elsevier Ltd</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>20120101</creationdate><title>Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs</title><author>Kumar, Ajay ; Shah, Bhahwal A. ; Singh, Samar ; Hamid, Abid ; Singh, Shashank K. ; Sethi, Vijay K. ; Saxena, Ajit K. ; Singh, Jaswant ; Taneja, Subhash C.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c385t-48c7c37fc75123e60f1624f1e9e8a73ddfd58114e4cb211252b86bf092bc1ada3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Acyl derivatives</topic><topic>Anti-cancer</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Boswellic acids</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation</topic><topic>Drug Design</topic><topic>Drug Screening Assays, Antitumor - methods</topic><topic>Flow Cytometry - methods</topic><topic>HL-60 Cells</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Models, Chemical</topic><topic>NF-kappa B - metabolism</topic><topic>NF-κB</topic><topic>Pharmacology. Drug treatments</topic><topic>Phosphorylation</topic><topic>STAT</topic><topic>STAT Transcription Factors - metabolism</topic><topic>Triterpenes - chemistry</topic><topic>Triterpenes - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumar, Ajay</creatorcontrib><creatorcontrib>Shah, Bhahwal A.</creatorcontrib><creatorcontrib>Singh, Samar</creatorcontrib><creatorcontrib>Hamid, Abid</creatorcontrib><creatorcontrib>Singh, Shashank K.</creatorcontrib><creatorcontrib>Sethi, Vijay K.</creatorcontrib><creatorcontrib>Saxena, Ajit K.</creatorcontrib><creatorcontrib>Singh, Jaswant</creatorcontrib><creatorcontrib>Taneja, Subhash C.</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>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kumar, Ajay</au><au>Shah, Bhahwal A.</au><au>Singh, Samar</au><au>Hamid, Abid</au><au>Singh, Shashank K.</au><au>Sethi, Vijay K.</au><au>Saxena, Ajit K.</au><au>Singh, Jaswant</au><au>Taneja, Subhash C.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2012-01-01</date><risdate>2012</risdate><volume>22</volume><issue>1</issue><spage>431</spage><epage>435</epage><pages>431-435</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Acyl derivatives of boswellic acids including their epimers were synthesized and screened against a panel of cancer cell lines. One of the lead compounds was found to be an inhibitor of NF-κB and STAT proteins.
Boswellic acid acylates including their epimers were synthesized and screened against a panel of human cancer cell lines. They exhibited a range of cytotoxicity against various human cancer cell lines thereby leading to the development of a possible SAR. One of the identified lead compounds was found to be an inhibitor of the NF-κB and STAT proteins, warranting further investigations to be developed into a potential anticancer lead.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>22123322</pmid><doi>10.1016/j.bmcl.2011.10.112</doi><tpages>5</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.431-435 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Acyl derivatives Anti-cancer Antineoplastic Agents - pharmacology Biological and medical sciences Boswellic acids Cell Line, Tumor Cell Proliferation Drug Design Drug Screening Assays, Antitumor - methods Flow Cytometry - methods HL-60 Cells Humans Medical sciences Models, Chemical NF-kappa B - metabolism NF-κB Pharmacology. Drug treatments Phosphorylation STAT STAT Transcription Factors - metabolism Triterpenes - chemistry Triterpenes - pharmacology |
| title | Acyl derivatives of boswellic acids as inhibitors of NF-κB and STATs |
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