Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors
A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure–activity relationships resulted in compounds that are potent in vitro. In addition, the bes...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2013-01, Vol.23 (1), p.179-182 |
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| container_end_page | 182 |
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| container_issue | 1 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 23 |
| creator | Li, Yanyang Zhou, Yan Qian, Pengyu Wang, Yongzhen Jiang, Falong Yao, Zhenglin Hu, Wenxiang Zhao, Yanjin Li, Shuxin |
| description | A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors.
A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure–activity relationships resulted in compounds that are potent in vitro. In addition, the best compound 1a exhibited an acceptable pharmacokinetic profile with bioavailability in rat of 81% and could be considered as a candidate compound for further development. |
| doi_str_mv | 10.1016/j.bmcl.2012.10.114 |
| format | Article |
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A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure–activity relationships resulted in compounds that are potent in vitro. In addition, the best compound 1a exhibited an acceptable pharmacokinetic profile with bioavailability in rat of 81% and could be considered as a candidate compound for further development.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2012.10.114</identifier><identifier>PMID: 23206867</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - pharmacokinetics ; Antineoplastic Agents - toxicity ; Antiproliferative activity ; Benzamide derivatives ; benzamides ; Benzamides - chemical synthesis ; Benzamides - chemistry ; Benzamides - pharmacokinetics ; Benzamides - toxicity ; Bioavailability ; Cell Line, Tumor ; Drug Design ; Drug Evaluation, Preclinical ; Drug Screening Assays, Antitumor ; Half-Life ; HCT116 Cells ; HDAC ; Histone Deacetylase Inhibitors - chemical synthesis ; Histone Deacetylase Inhibitors - pharmacokinetics ; Histone Deacetylase Inhibitors - toxicity ; Histone Deacetylases - chemistry ; Histone Deacetylases - metabolism ; Humans ; MCF-7 Cells ; pharmacokinetics ; Pyrimidines - chemical synthesis ; Pyrimidines - pharmacokinetics ; Pyrimidines - toxicity ; Rats ; Structure-Activity Relationship ; structure-activity relationships</subject><ispartof>Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.179-182</ispartof><rights>2012 Elsevier Ltd</rights><rights>Copyright © 2012 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c380t-bf68110c3fe0c6751f7258f912e1a74cbb637221f1b4946f80ec948c8f3564863</citedby><cites>FETCH-LOGICAL-c380t-bf68110c3fe0c6751f7258f912e1a74cbb637221f1b4946f80ec948c8f3564863</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2012.10.114$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,4022,27922,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23206867$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Yanyang</creatorcontrib><creatorcontrib>Zhou, Yan</creatorcontrib><creatorcontrib>Qian, Pengyu</creatorcontrib><creatorcontrib>Wang, Yongzhen</creatorcontrib><creatorcontrib>Jiang, Falong</creatorcontrib><creatorcontrib>Yao, Zhenglin</creatorcontrib><creatorcontrib>Hu, Wenxiang</creatorcontrib><creatorcontrib>Zhao, Yanjin</creatorcontrib><creatorcontrib>Li, Shuxin</creatorcontrib><title>Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors.
A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure–activity relationships resulted in compounds that are potent in vitro. In addition, the best compound 1a exhibited an acceptable pharmacokinetic profile with bioavailability in rat of 81% and could be considered as a candidate compound for further development.</description><subject>Animals</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacokinetics</subject><subject>Antineoplastic Agents - toxicity</subject><subject>Antiproliferative activity</subject><subject>Benzamide derivatives</subject><subject>benzamides</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacokinetics</subject><subject>Benzamides - toxicity</subject><subject>Bioavailability</subject><subject>Cell Line, Tumor</subject><subject>Drug Design</subject><subject>Drug Evaluation, Preclinical</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Half-Life</subject><subject>HCT116 Cells</subject><subject>HDAC</subject><subject>Histone Deacetylase Inhibitors - chemical synthesis</subject><subject>Histone Deacetylase Inhibitors - pharmacokinetics</subject><subject>Histone Deacetylase Inhibitors - toxicity</subject><subject>Histone Deacetylases - chemistry</subject><subject>Histone Deacetylases - metabolism</subject><subject>Humans</subject><subject>MCF-7 Cells</subject><subject>pharmacokinetics</subject><subject>Pyrimidines - chemical synthesis</subject><subject>Pyrimidines - pharmacokinetics</subject><subject>Pyrimidines - toxicity</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><subject>structure-activity relationships</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFu1DAQhi0EokvhBThAjj2QxeM4jiNxqbZAkSpxgJW4WbYzbr1K7GJnI5Wnx2ELR04zGn3za-Yj5DXQLVAQ7w9bM9lxyyiw7ToD_oRsgAteN5y2T8mG9oLWsuc_zsiLnA-UAqecPydnrGFUSNFtyP4Ks78N76r8EOa70udKh6EyPuKix-PsY6iiq0JccKwMhl968gPmasDkFz37pfQ6V9dXl7vKhztv_BxTfkmeOT1mfPVYz8n-08fvu-v65uvnL7vLm9o2ks61cUICUNs4pFZ0LbiOtdL1wBB0x60xoukYAweG91w4SdH2XFrpmlZwKZpzcnHKvU_x5xHzrCafLY6jDhiPWQHjVPayfF1QdkJtijkndOo--UmnBwVUrTrVQa061arzzwzWpTeP-Ucz4fBv5a-_Arw9AU5HpW-Tz2r_rSS0xXUDvKOF-HAisHhYPCaVrcdgcfAJ7ayG6P93wW__ao7B</recordid><startdate>20130101</startdate><enddate>20130101</enddate><creator>Li, Yanyang</creator><creator>Zhou, Yan</creator><creator>Qian, Pengyu</creator><creator>Wang, Yongzhen</creator><creator>Jiang, Falong</creator><creator>Yao, Zhenglin</creator><creator>Hu, Wenxiang</creator><creator>Zhao, Yanjin</creator><creator>Li, Shuxin</creator><general>Elsevier Ltd</general><scope>FBQ</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>20130101</creationdate><title>Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors</title><author>Li, Yanyang ; Zhou, Yan ; Qian, Pengyu ; Wang, Yongzhen ; Jiang, Falong ; Yao, Zhenglin ; Hu, Wenxiang ; Zhao, Yanjin ; Li, Shuxin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c380t-bf68110c3fe0c6751f7258f912e1a74cbb637221f1b4946f80ec948c8f3564863</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Animals</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - pharmacokinetics</topic><topic>Antineoplastic Agents - toxicity</topic><topic>Antiproliferative activity</topic><topic>Benzamide derivatives</topic><topic>benzamides</topic><topic>Benzamides - chemical synthesis</topic><topic>Benzamides - chemistry</topic><topic>Benzamides - pharmacokinetics</topic><topic>Benzamides - toxicity</topic><topic>Bioavailability</topic><topic>Cell Line, Tumor</topic><topic>Drug Design</topic><topic>Drug Evaluation, Preclinical</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Half-Life</topic><topic>HCT116 Cells</topic><topic>HDAC</topic><topic>Histone Deacetylase Inhibitors - chemical synthesis</topic><topic>Histone Deacetylase Inhibitors - pharmacokinetics</topic><topic>Histone Deacetylase Inhibitors - toxicity</topic><topic>Histone Deacetylases - chemistry</topic><topic>Histone Deacetylases - metabolism</topic><topic>Humans</topic><topic>MCF-7 Cells</topic><topic>pharmacokinetics</topic><topic>Pyrimidines - chemical synthesis</topic><topic>Pyrimidines - pharmacokinetics</topic><topic>Pyrimidines - toxicity</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><topic>structure-activity relationships</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Yanyang</creatorcontrib><creatorcontrib>Zhou, Yan</creatorcontrib><creatorcontrib>Qian, Pengyu</creatorcontrib><creatorcontrib>Wang, Yongzhen</creatorcontrib><creatorcontrib>Jiang, Falong</creatorcontrib><creatorcontrib>Yao, Zhenglin</creatorcontrib><creatorcontrib>Hu, Wenxiang</creatorcontrib><creatorcontrib>Zhao, Yanjin</creatorcontrib><creatorcontrib>Li, Shuxin</creatorcontrib><collection>AGRIS</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>Li, Yanyang</au><au>Zhou, Yan</au><au>Qian, Pengyu</au><au>Wang, Yongzhen</au><au>Jiang, Falong</au><au>Yao, Zhenglin</au><au>Hu, Wenxiang</au><au>Zhao, Yanjin</au><au>Li, Shuxin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2013-01-01</date><risdate>2013</risdate><volume>23</volume><issue>1</issue><spage>179</spage><epage>182</epage><pages>179-182</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors.
A series of novel benzamides derivatives was designed and synthesized as HDAC inhibitors. Exploration of the structure–activity relationships resulted in compounds that are potent in vitro. In addition, the best compound 1a exhibited an acceptable pharmacokinetic profile with bioavailability in rat of 81% and could be considered as a candidate compound for further development.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>23206867</pmid><doi>10.1016/j.bmcl.2012.10.114</doi><tpages>4</tpages></addata></record> |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - toxicity Antiproliferative activity Benzamide derivatives benzamides Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacokinetics Benzamides - toxicity Bioavailability Cell Line, Tumor Drug Design Drug Evaluation, Preclinical Drug Screening Assays, Antitumor Half-Life HCT116 Cells HDAC Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - pharmacokinetics Histone Deacetylase Inhibitors - toxicity Histone Deacetylases - chemistry Histone Deacetylases - metabolism Humans MCF-7 Cells pharmacokinetics Pyrimidines - chemical synthesis Pyrimidines - pharmacokinetics Pyrimidines - toxicity Rats Structure-Activity Relationship structure-activity relationships |
| title | Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors |
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