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Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors
[Display omitted] Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and exce...
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| Published in: | Bioorganic & medicinal chemistry letters 2016-06, Vol.26 (11), p.2735-2738 |
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| Main Authors: | , , , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c389t-5e11acc484423260bcf73818a0e8ac6e4093ace0df45975aab994dc4c5a94e6c3 |
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| cites | cdi_FETCH-LOGICAL-c389t-5e11acc484423260bcf73818a0e8ac6e4093ace0df45975aab994dc4c5a94e6c3 |
| container_end_page | 2738 |
| container_issue | 11 |
| container_start_page | 2735 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 26 |
| creator | Tian, Yuan Ma, Yao Gibeau, Craig R. Lahue, Brian R. Shipps, Gerald W. Strickland, Corey Bogen, Stéphane L. |
| description | [Display omitted]
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles. |
| doi_str_mv | 10.1016/j.bmcl.2016.03.078 |
| format | article |
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Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2016.03.078</identifier><identifier>PMID: 27080185</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Dose-Response Relationship, Drug ; hDM2 ; Humans ; Leucine - chemistry ; Models, Molecular ; Molecular Structure ; p53 ; Piperidines - chemical synthesis ; Piperidines - chemistry ; Piperidines - pharmacology ; Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors ; Proto-Oncogene Proteins c-mdm2 - metabolism ; SAR ; Structure-Activity Relationship ; Tumor Suppressor Protein p53 - antagonists & inhibitors ; Tumor Suppressor Protein p53 - metabolism</subject><ispartof>Bioorganic & medicinal chemistry letters, 2016-06, Vol.26 (11), p.2735-2738</ispartof><rights>2016 Elsevier Ltd</rights><rights>Copyright © 2016 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c389t-5e11acc484423260bcf73818a0e8ac6e4093ace0df45975aab994dc4c5a94e6c3</citedby><cites>FETCH-LOGICAL-c389t-5e11acc484423260bcf73818a0e8ac6e4093ace0df45975aab994dc4c5a94e6c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27080185$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tian, Yuan</creatorcontrib><creatorcontrib>Ma, Yao</creatorcontrib><creatorcontrib>Gibeau, Craig R.</creatorcontrib><creatorcontrib>Lahue, Brian R.</creatorcontrib><creatorcontrib>Shipps, Gerald W.</creatorcontrib><creatorcontrib>Strickland, Corey</creatorcontrib><creatorcontrib>Bogen, Stéphane L.</creatorcontrib><title>Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.</description><subject>Dose-Response Relationship, Drug</subject><subject>hDM2</subject><subject>Humans</subject><subject>Leucine - chemistry</subject><subject>Models, Molecular</subject><subject>Molecular Structure</subject><subject>p53</subject><subject>Piperidines - chemical synthesis</subject><subject>Piperidines - chemistry</subject><subject>Piperidines - pharmacology</subject><subject>Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors</subject><subject>Proto-Oncogene Proteins c-mdm2 - metabolism</subject><subject>SAR</subject><subject>Structure-Activity Relationship</subject><subject>Tumor Suppressor Protein p53 - antagonists & inhibitors</subject><subject>Tumor Suppressor Protein p53 - metabolism</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><recordid>eNqFkbmOFDEQQC3Eih0WfoAAOSTpptw-2i2RoF0uaVYEgERmud3VGo_6wsdIk_EP_OF-CT3MQshGVcGrF9Qj5AWDkgFTr_dlO7qhrNa9BF5CrR-RDRNKFFyAfEw20CgodCO-X5KnMe4BmAAhnpDLqgYNTMsNiV9SyC7lgHc_f1mX_MGnIw042OTnKe78QmPK3ZHOPRVFzG1MPuWEHV38gsF3fsJIbaJbzJWi4-wx_YGn-YADXSRfvbub24r6aedbn-YQn5GL3g4Rn9_PK_Lt_buv1x-L7ecPn67fbgvHdZMKiYxZ54QWouKVgtb1NddMW0BtnUIBDbcOoeuFbGppbds0onPCSdsIVI5fkVdn7xLmHxljMqOPDofBTjjnaJgGrWolpXgYrbWSrBY1rGh1Rl2YYwzYmyX40YajYWBOXczenLqYUxcD3Kxd1qOX9_7cjtj9O_kbYgXenAFcH3LwGEx0HieHnQ_okulm_z__bzccocc</recordid><startdate>20160601</startdate><enddate>20160601</enddate><creator>Tian, Yuan</creator><creator>Ma, Yao</creator><creator>Gibeau, Craig R.</creator><creator>Lahue, Brian R.</creator><creator>Shipps, Gerald W.</creator><creator>Strickland, Corey</creator><creator>Bogen, Stéphane L.</creator><general>Elsevier Ltd</general><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><scope>7QO</scope><scope>7TO</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope></search><sort><creationdate>20160601</creationdate><title>Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors</title><author>Tian, Yuan ; Ma, Yao ; Gibeau, Craig R. ; Lahue, Brian R. ; Shipps, Gerald W. ; Strickland, Corey ; Bogen, Stéphane L.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c389t-5e11acc484423260bcf73818a0e8ac6e4093ace0df45975aab994dc4c5a94e6c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Dose-Response Relationship, Drug</topic><topic>hDM2</topic><topic>Humans</topic><topic>Leucine - chemistry</topic><topic>Models, Molecular</topic><topic>Molecular Structure</topic><topic>p53</topic><topic>Piperidines - chemical synthesis</topic><topic>Piperidines - chemistry</topic><topic>Piperidines - pharmacology</topic><topic>Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors</topic><topic>Proto-Oncogene Proteins c-mdm2 - metabolism</topic><topic>SAR</topic><topic>Structure-Activity Relationship</topic><topic>Tumor Suppressor Protein p53 - antagonists & inhibitors</topic><topic>Tumor Suppressor Protein p53 - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tian, Yuan</creatorcontrib><creatorcontrib>Ma, Yao</creatorcontrib><creatorcontrib>Gibeau, Craig R.</creatorcontrib><creatorcontrib>Lahue, Brian R.</creatorcontrib><creatorcontrib>Shipps, Gerald W.</creatorcontrib><creatorcontrib>Strickland, Corey</creatorcontrib><creatorcontrib>Bogen, Stéphane L.</creatorcontrib><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><collection>Biotechnology Research Abstracts</collection><collection>Oncogenes and Growth Factors Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tian, Yuan</au><au>Ma, Yao</au><au>Gibeau, Craig R.</au><au>Lahue, Brian R.</au><au>Shipps, Gerald W.</au><au>Strickland, Corey</au><au>Bogen, Stéphane L.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2016-06-01</date><risdate>2016</risdate><volume>26</volume><issue>11</issue><spage>2735</spage><epage>2738</epage><pages>2735-2738</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>27080185</pmid><doi>10.1016/j.bmcl.2016.03.078</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2016-06, Vol.26 (11), p.2735-2738 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1808676554 |
| source | ScienceDirect Freedom Collection |
| subjects | Dose-Response Relationship, Drug hDM2 Humans Leucine - chemistry Models, Molecular Molecular Structure p53 Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors Proto-Oncogene Proteins c-mdm2 - metabolism SAR Structure-Activity Relationship Tumor Suppressor Protein p53 - antagonists & inhibitors Tumor Suppressor Protein p53 - metabolism |
| title | Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors |
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