Loading…
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III
Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 ( 22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.
Saved in:
| Published in: | Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (10), p.3155-3157 |
|---|---|
| Main Authors: | , , , , , , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
| Subjects: | |
| Citations: | Items that this one cites Items that cite this one |
| Online Access: | Get full text |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| cited_by | cdi_FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443 |
|---|---|
| cites | cdi_FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443 |
| container_end_page | 3157 |
| container_issue | 10 |
| container_start_page | 3155 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 20 |
| creator | Shen, Yongchun Boivin, Roch Yoneda, Naoki Du, Hong Schiller, Shawn Matsushima, Tomohiro Goto, Masaki Shirota, Hiroshi Gusovsky, Fabian Lemelin, Charles Jiang, Yimin Zhang, Zhiyi Pelletier, Robert Ikemori-Kawada, Megumi Kawakami, Yoshiyuki Inoue, Atsushi Schnaderbeck, Matthew Wang, Yuan |
| description | Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (
22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to
N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays. |
| doi_str_mv | 10.1016/j.bmcl.2010.03.087 |
| format | article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_733943447</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X10004282</els_id><sourcerecordid>733943447</sourcerecordid><originalsourceid>FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443</originalsourceid><addsrcrecordid>eNp9kM-LEzEUx4Mobl39BzxILuJlp778mEwDXpZ1VwsFLwriJaRvXiBlZlKT6UL_e1Na9banB18-79eHsbcClgKE-bhbbkcclhJqAGoJq-4ZWwhtdKM0tM_ZAqyBZmX1zyv2qpQdgNCg9Ut2JUFZa_RqweLnWDA9Uj7yFLif5tjEKQx-HP2caohDnCL6gaOf-tj7mfi9qRtveJzKPmbqechp5JlKyngcIvLB45wm4ptN80sYDY284ev1-jV7EfxQ6M2lXrMfD_ff7742m29f1ne3mwZ1K-YmeOx8h50lGbQAaVuJwipLRgTEYDqCtu8FdOBbuVJt57feqJZ8D8EordU1-3Ceu8_p94HK7Mb6Ig2DnygdiuuUsrqCXSXlmcScSskU3D7H0eejE-BOht3OnQy7k2EHylXDtendZfxhO1L_r-Wv0gq8vwC-VHEh-wlj-c_JlTVKmsp9OnNUZTxGyq5gpAmpr1Zxdn2KT93xB0bTl9k</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>733943447</pqid></control><display><type>article</type><title>Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III</title><source>ScienceDirect Freedom Collection 2022-2024</source><creator>Shen, Yongchun ; Boivin, Roch ; Yoneda, Naoki ; Du, Hong ; Schiller, Shawn ; Matsushima, Tomohiro ; Goto, Masaki ; Shirota, Hiroshi ; Gusovsky, Fabian ; Lemelin, Charles ; Jiang, Yimin ; Zhang, Zhiyi ; Pelletier, Robert ; Ikemori-Kawada, Megumi ; Kawakami, Yoshiyuki ; Inoue, Atsushi ; Schnaderbeck, Matthew ; Wang, Yuan</creator><creatorcontrib>Shen, Yongchun ; Boivin, Roch ; Yoneda, Naoki ; Du, Hong ; Schiller, Shawn ; Matsushima, Tomohiro ; Goto, Masaki ; Shirota, Hiroshi ; Gusovsky, Fabian ; Lemelin, Charles ; Jiang, Yimin ; Zhang, Zhiyi ; Pelletier, Robert ; Ikemori-Kawada, Megumi ; Kawakami, Yoshiyuki ; Inoue, Atsushi ; Schnaderbeck, Matthew ; Wang, Yuan</creatorcontrib><description>Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (
22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to
N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.03.087</identifier><identifier>PMID: 20399648</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Administration, Oral ; Animals ; Anti-inflammatory ; Anti-Inflammatory Agents - chemical synthesis ; Anti-Inflammatory Agents - chemistry ; Anti-Inflammatory Agents - pharmacokinetics ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Drug Discovery ; f152A1 ; Lactones - chemical synthesis ; Lactones - chemistry ; Lactones - pharmacokinetics ; LL-Z1640-2 ; Medical sciences ; Mice ; Pharmacology. Drug treatments ; Resorcylic lactone ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (10), p.3155-3157</ispartof><rights>2010 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright 2010 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443</citedby><cites>FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22896326$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20399648$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shen, Yongchun</creatorcontrib><creatorcontrib>Boivin, Roch</creatorcontrib><creatorcontrib>Yoneda, Naoki</creatorcontrib><creatorcontrib>Du, Hong</creatorcontrib><creatorcontrib>Schiller, Shawn</creatorcontrib><creatorcontrib>Matsushima, Tomohiro</creatorcontrib><creatorcontrib>Goto, Masaki</creatorcontrib><creatorcontrib>Shirota, Hiroshi</creatorcontrib><creatorcontrib>Gusovsky, Fabian</creatorcontrib><creatorcontrib>Lemelin, Charles</creatorcontrib><creatorcontrib>Jiang, Yimin</creatorcontrib><creatorcontrib>Zhang, Zhiyi</creatorcontrib><creatorcontrib>Pelletier, Robert</creatorcontrib><creatorcontrib>Ikemori-Kawada, Megumi</creatorcontrib><creatorcontrib>Kawakami, Yoshiyuki</creatorcontrib><creatorcontrib>Inoue, Atsushi</creatorcontrib><creatorcontrib>Schnaderbeck, Matthew</creatorcontrib><creatorcontrib>Wang, Yuan</creatorcontrib><title>Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (
22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to
N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Anti-inflammatory</subject><subject>Anti-Inflammatory Agents - chemical synthesis</subject><subject>Anti-Inflammatory Agents - chemistry</subject><subject>Anti-Inflammatory Agents - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Drug Discovery</subject><subject>f152A1</subject><subject>Lactones - chemical synthesis</subject><subject>Lactones - chemistry</subject><subject>Lactones - pharmacokinetics</subject><subject>LL-Z1640-2</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Pharmacology. Drug treatments</subject><subject>Resorcylic lactone</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><recordid>eNp9kM-LEzEUx4Mobl39BzxILuJlp778mEwDXpZ1VwsFLwriJaRvXiBlZlKT6UL_e1Na9banB18-79eHsbcClgKE-bhbbkcclhJqAGoJq-4ZWwhtdKM0tM_ZAqyBZmX1zyv2qpQdgNCg9Ut2JUFZa_RqweLnWDA9Uj7yFLif5tjEKQx-HP2caohDnCL6gaOf-tj7mfi9qRtveJzKPmbqechp5JlKyngcIvLB45wm4ptN80sYDY284ev1-jV7EfxQ6M2lXrMfD_ff7742m29f1ne3mwZ1K-YmeOx8h50lGbQAaVuJwipLRgTEYDqCtu8FdOBbuVJt57feqJZ8D8EordU1-3Ceu8_p94HK7Mb6Ig2DnygdiuuUsrqCXSXlmcScSskU3D7H0eejE-BOht3OnQy7k2EHylXDtendZfxhO1L_r-Wv0gq8vwC-VHEh-wlj-c_JlTVKmsp9OnNUZTxGyq5gpAmpr1Zxdn2KT93xB0bTl9k</recordid><startdate>20100515</startdate><enddate>20100515</enddate><creator>Shen, Yongchun</creator><creator>Boivin, Roch</creator><creator>Yoneda, Naoki</creator><creator>Du, Hong</creator><creator>Schiller, Shawn</creator><creator>Matsushima, Tomohiro</creator><creator>Goto, Masaki</creator><creator>Shirota, Hiroshi</creator><creator>Gusovsky, Fabian</creator><creator>Lemelin, Charles</creator><creator>Jiang, Yimin</creator><creator>Zhang, Zhiyi</creator><creator>Pelletier, Robert</creator><creator>Ikemori-Kawada, Megumi</creator><creator>Kawakami, Yoshiyuki</creator><creator>Inoue, Atsushi</creator><creator>Schnaderbeck, Matthew</creator><creator>Wang, Yuan</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>20100515</creationdate><title>Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III</title><author>Shen, Yongchun ; Boivin, Roch ; Yoneda, Naoki ; Du, Hong ; Schiller, Shawn ; Matsushima, Tomohiro ; Goto, Masaki ; Shirota, Hiroshi ; Gusovsky, Fabian ; Lemelin, Charles ; Jiang, Yimin ; Zhang, Zhiyi ; Pelletier, Robert ; Ikemori-Kawada, Megumi ; Kawakami, Yoshiyuki ; Inoue, Atsushi ; Schnaderbeck, Matthew ; Wang, Yuan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Anti-inflammatory</topic><topic>Anti-Inflammatory Agents - chemical synthesis</topic><topic>Anti-Inflammatory Agents - chemistry</topic><topic>Anti-Inflammatory Agents - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Drug Discovery</topic><topic>f152A1</topic><topic>Lactones - chemical synthesis</topic><topic>Lactones - chemistry</topic><topic>Lactones - pharmacokinetics</topic><topic>LL-Z1640-2</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Pharmacology. Drug treatments</topic><topic>Resorcylic lactone</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shen, Yongchun</creatorcontrib><creatorcontrib>Boivin, Roch</creatorcontrib><creatorcontrib>Yoneda, Naoki</creatorcontrib><creatorcontrib>Du, Hong</creatorcontrib><creatorcontrib>Schiller, Shawn</creatorcontrib><creatorcontrib>Matsushima, Tomohiro</creatorcontrib><creatorcontrib>Goto, Masaki</creatorcontrib><creatorcontrib>Shirota, Hiroshi</creatorcontrib><creatorcontrib>Gusovsky, Fabian</creatorcontrib><creatorcontrib>Lemelin, Charles</creatorcontrib><creatorcontrib>Jiang, Yimin</creatorcontrib><creatorcontrib>Zhang, Zhiyi</creatorcontrib><creatorcontrib>Pelletier, Robert</creatorcontrib><creatorcontrib>Ikemori-Kawada, Megumi</creatorcontrib><creatorcontrib>Kawakami, Yoshiyuki</creatorcontrib><creatorcontrib>Inoue, Atsushi</creatorcontrib><creatorcontrib>Schnaderbeck, Matthew</creatorcontrib><creatorcontrib>Wang, Yuan</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>Shen, Yongchun</au><au>Boivin, Roch</au><au>Yoneda, Naoki</au><au>Du, Hong</au><au>Schiller, Shawn</au><au>Matsushima, Tomohiro</au><au>Goto, Masaki</au><au>Shirota, Hiroshi</au><au>Gusovsky, Fabian</au><au>Lemelin, Charles</au><au>Jiang, Yimin</au><au>Zhang, Zhiyi</au><au>Pelletier, Robert</au><au>Ikemori-Kawada, Megumi</au><au>Kawakami, Yoshiyuki</au><au>Inoue, Atsushi</au><au>Schnaderbeck, Matthew</au><au>Wang, Yuan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-05-15</date><risdate>2010</risdate><volume>20</volume><issue>10</issue><spage>3155</spage><epage>3157</epage><pages>3155-3157</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (
22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to
N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>20399648</pmid><doi>10.1016/j.bmcl.2010.03.087</doi><tpages>3</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (10), p.3155-3157 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_733943447 |
| source | ScienceDirect Freedom Collection 2022-2024 |
| subjects | Administration, Oral Animals Anti-inflammatory Anti-Inflammatory Agents - chemical synthesis Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacokinetics Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Drug Discovery f152A1 Lactones - chemical synthesis Lactones - chemistry Lactones - pharmacokinetics LL-Z1640-2 Medical sciences Mice Pharmacology. Drug treatments Resorcylic lactone Structure-Activity Relationship |
| title | Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III |
| url | http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-06T09%3A47%3A01IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Discovery%20of%20anti-inflammatory%20clinical%20candidate%20E6201,%20inspired%20from%20resorcylic%20lactone%20LL-Z1640-2,%20III&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Shen,%20Yongchun&rft.date=2010-05-15&rft.volume=20&rft.issue=10&rft.spage=3155&rft.epage=3157&rft.pages=3155-3157&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2010.03.087&rft_dat=%3Cproquest_cross%3E733943447%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c451t-fac7a7c79e2f4102952c1939e61fccf67e05dd1070a528357aba635ead0f63443%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=733943447&rft_id=info:pmid/20399648&rfr_iscdi=true |