Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties
We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2012-11, Vol.22 (21), p.6750-6755 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 6755 |
|---|---|
| container_issue | 21 |
| container_start_page | 6750 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 22 |
| creator | Chang, Dong-Jo Lee, Sujin Jang, Jaebong Kim, Soon-Ok Kim, Wan-Joo Suh, Young-Ger |
| description | We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in vitro activity (IC50: 5nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema model and in the local lymph node assay (LLNA). Analog 14 also revealed a good oral bioavailability (F: 67.3%) in BALB/c mice. |
| doi_str_mv | 10.1016/j.bmcl.2012.08.068 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1125238624</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X12010797</els_id><sourcerecordid>1125238624</sourcerecordid><originalsourceid>FETCH-LOGICAL-c419t-218261962b6ae168f3993164f24f27c0351a0dc7bf971b00e6505a7d3165585a3</originalsourceid><addsrcrecordid>eNqNkUGr1DAQx4Movn1Pv4AH6UXw0jqTJtkUvMhTnwsP9KDgLaTplM3aNjVpV_z2ZtlVbyIEhgy__yTMj7FnCBUCqleHqh3dUHFAXoGuQOkHbINCibIWIB-yDTQKSt2Ir1fsOqUDAAoQ4jG74jXgVmu5YcMnG5dit6uKt3SkIcwjTUsR-mIK-Vq4MLi9d36isqPoj9QVfhzXKaR1niOlZKclFT_8ss_9OYYTMO9tHK0L33Jq8a7I7Zni4ik9YY96OyR6eqk37Mv7d59vP5T3H-92t2_uSyewWUqOmitsFG-VJVS6r5umRiV6ns_WQS3RQue2bd9ssQUgJUHabZcZKbW09Q17eZ6bn_6-UlrM6JOjYbAThTUZRC55rRUX_4EirwVXoDPKz6iLIaVIvZmjH238aRDMSYg5mJMQcxJiQJssJIeeX-av7Ujdn8hvAxl4cQFscnboo52cT385JUWDEjL3-sxRXtzRUzTJeZocdT6SW0wX_L_-8Qt7YKmR</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1112342608</pqid></control><display><type>article</type><title>Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals Complete</source><creator>Chang, Dong-Jo ; Lee, Sujin ; Jang, Jaebong ; Kim, Soon-Ok ; Kim, Wan-Joo ; Suh, Young-Ger</creator><creatorcontrib>Chang, Dong-Jo ; Lee, Sujin ; Jang, Jaebong ; Kim, Soon-Ok ; Kim, Wan-Joo ; Suh, Young-Ger</creatorcontrib><description>We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in vitro activity (IC50: 5nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema model and in the local lymph node assay (LLNA). Analog 14 also revealed a good oral bioavailability (F: 67.3%) in BALB/c mice.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2012.08.068</identifier><identifier>PMID: 23017885</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Administration, Oral ; Animals ; Arthritis ; Arthritis - drug therapy ; Autoimmune disease ; Bioavailability ; Biological and medical sciences ; Biological Availability ; Colchicine ; Colchicine - chemistry ; Colchicine - pharmacokinetics ; Colchicine - pharmacology ; Cyclosporine A (CsA) ; Disease Models, Animal ; Edema ; Immunosuppressant ; Immunosuppressive agents ; Immunosuppressive Agents - chemistry ; Immunosuppressive Agents - pharmacokinetics ; Immunosuppressive Agents - pharmacology ; Inhibitory Concentration 50 ; Local lymph node assay ; Medical sciences ; Mice ; Mice, Inbred BALB C ; Mixed-lymphocyte reaction (MLR) ; Molecular Structure ; Pharmacokinetics ; Pharmacology. Drug treatments ; Rejection of organ-transplantation</subject><ispartof>Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6750-6755</ispartof><rights>2012 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2012 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c419t-218261962b6ae168f3993164f24f27c0351a0dc7bf971b00e6505a7d3165585a3</citedby><cites>FETCH-LOGICAL-c419t-218261962b6ae168f3993164f24f27c0351a0dc7bf971b00e6505a7d3165585a3</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.2012.08.068$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26549150$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23017885$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chang, Dong-Jo</creatorcontrib><creatorcontrib>Lee, Sujin</creatorcontrib><creatorcontrib>Jang, Jaebong</creatorcontrib><creatorcontrib>Kim, Soon-Ok</creatorcontrib><creatorcontrib>Kim, Wan-Joo</creatorcontrib><creatorcontrib>Suh, Young-Ger</creatorcontrib><title>Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in vitro activity (IC50: 5nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema model and in the local lymph node assay (LLNA). Analog 14 also revealed a good oral bioavailability (F: 67.3%) in BALB/c mice.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Arthritis</subject><subject>Arthritis - drug therapy</subject><subject>Autoimmune disease</subject><subject>Bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Colchicine</subject><subject>Colchicine - chemistry</subject><subject>Colchicine - pharmacokinetics</subject><subject>Colchicine - pharmacology</subject><subject>Cyclosporine A (CsA)</subject><subject>Disease Models, Animal</subject><subject>Edema</subject><subject>Immunosuppressant</subject><subject>Immunosuppressive agents</subject><subject>Immunosuppressive Agents - chemistry</subject><subject>Immunosuppressive Agents - pharmacokinetics</subject><subject>Immunosuppressive Agents - pharmacology</subject><subject>Inhibitory Concentration 50</subject><subject>Local lymph node assay</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>Mixed-lymphocyte reaction (MLR)</subject><subject>Molecular Structure</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Rejection of organ-transplantation</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>eNqNkUGr1DAQx4Movn1Pv4AH6UXw0jqTJtkUvMhTnwsP9KDgLaTplM3aNjVpV_z2ZtlVbyIEhgy__yTMj7FnCBUCqleHqh3dUHFAXoGuQOkHbINCibIWIB-yDTQKSt2Ir1fsOqUDAAoQ4jG74jXgVmu5YcMnG5dit6uKt3SkIcwjTUsR-mIK-Vq4MLi9d36isqPoj9QVfhzXKaR1niOlZKclFT_8ss_9OYYTMO9tHK0L33Jq8a7I7Zni4ik9YY96OyR6eqk37Mv7d59vP5T3H-92t2_uSyewWUqOmitsFG-VJVS6r5umRiV6ns_WQS3RQue2bd9ssQUgJUHabZcZKbW09Q17eZ6bn_6-UlrM6JOjYbAThTUZRC55rRUX_4EirwVXoDPKz6iLIaVIvZmjH238aRDMSYg5mJMQcxJiQJssJIeeX-av7Ujdn8hvAxl4cQFscnboo52cT385JUWDEjL3-sxRXtzRUzTJeZocdT6SW0wX_L_-8Qt7YKmR</recordid><startdate>20121101</startdate><enddate>20121101</enddate><creator>Chang, Dong-Jo</creator><creator>Lee, Sujin</creator><creator>Jang, Jaebong</creator><creator>Kim, Soon-Ok</creator><creator>Kim, Wan-Joo</creator><creator>Suh, Young-Ger</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><scope>7QO</scope><scope>7T5</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope></search><sort><creationdate>20121101</creationdate><title>Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties</title><author>Chang, Dong-Jo ; Lee, Sujin ; Jang, Jaebong ; Kim, Soon-Ok ; Kim, Wan-Joo ; Suh, Young-Ger</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c419t-218261962b6ae168f3993164f24f27c0351a0dc7bf971b00e6505a7d3165585a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Arthritis</topic><topic>Arthritis - drug therapy</topic><topic>Autoimmune disease</topic><topic>Bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Colchicine</topic><topic>Colchicine - chemistry</topic><topic>Colchicine - pharmacokinetics</topic><topic>Colchicine - pharmacology</topic><topic>Cyclosporine A (CsA)</topic><topic>Disease Models, Animal</topic><topic>Edema</topic><topic>Immunosuppressant</topic><topic>Immunosuppressive agents</topic><topic>Immunosuppressive Agents - chemistry</topic><topic>Immunosuppressive Agents - pharmacokinetics</topic><topic>Immunosuppressive Agents - pharmacology</topic><topic>Inhibitory Concentration 50</topic><topic>Local lymph node assay</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred BALB C</topic><topic>Mixed-lymphocyte reaction (MLR)</topic><topic>Molecular Structure</topic><topic>Pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Rejection of organ-transplantation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chang, Dong-Jo</creatorcontrib><creatorcontrib>Lee, Sujin</creatorcontrib><creatorcontrib>Jang, Jaebong</creatorcontrib><creatorcontrib>Kim, Soon-Ok</creatorcontrib><creatorcontrib>Kim, Wan-Joo</creatorcontrib><creatorcontrib>Suh, Young-Ger</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><collection>Biotechnology Research Abstracts</collection><collection>Immunology 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>Chang, Dong-Jo</au><au>Lee, Sujin</au><au>Jang, Jaebong</au><au>Kim, Soon-Ok</au><au>Kim, Wan-Joo</au><au>Suh, Young-Ger</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2012-11-01</date><risdate>2012</risdate><volume>22</volume><issue>21</issue><spage>6750</spage><epage>6755</epage><pages>6750-6755</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in vitro activity (IC50: 5nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema model and in the local lymph node assay (LLNA). Analog 14 also revealed a good oral bioavailability (F: 67.3%) in BALB/c mice.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>23017885</pmid><doi>10.1016/j.bmcl.2012.08.068</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6750-6755 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1125238624 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Administration, Oral Animals Arthritis Arthritis - drug therapy Autoimmune disease Bioavailability Biological and medical sciences Biological Availability Colchicine Colchicine - chemistry Colchicine - pharmacokinetics Colchicine - pharmacology Cyclosporine A (CsA) Disease Models, Animal Edema Immunosuppressant Immunosuppressive agents Immunosuppressive Agents - chemistry Immunosuppressive Agents - pharmacokinetics Immunosuppressive Agents - pharmacology Inhibitory Concentration 50 Local lymph node assay Medical sciences Mice Mice, Inbred BALB C Mixed-lymphocyte reaction (MLR) Molecular Structure Pharmacokinetics Pharmacology. Drug treatments Rejection of organ-transplantation |
| title | Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-01T13%3A57%3A18IST&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=Part%20II.%20Development%20of%20novel%20colchicine-derived%20immunosuppressants%20with%20improved%20pharmacokinetic%20properties&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Chang,%20Dong-Jo&rft.date=2012-11-01&rft.volume=22&rft.issue=21&rft.spage=6750&rft.epage=6755&rft.pages=6750-6755&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2012.08.068&rft_dat=%3Cproquest_cross%3E1125238624%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1112342608&rft_id=info:pmid/23017885&rft_els_id=S0960894X12010797&rfr_iscdi=true |