Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)
[Display omitted] Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxa...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2015-10, Vol.25 (19), p.4265-4269 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Liu, Qingjie Batt, Douglas G. Lippy, Jonathan S. Surti, Neha Tebben, Andrew J. Muckelbauer, Jodi K. Chen, Lin An, Yongmi Chang, Chiehying Pokross, Matt Yang, Zheng Wang, Haiqing Burke, James R. Carter, Percy H. Tino, Joseph A. |
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Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2). |
| doi_str_mv | 10.1016/j.bmcl.2015.07.102 |
| format | Article |
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Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2015.07.102</identifier><identifier>PMID: 26320619</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>60 APPLIED LIFE SCIENCES ; Amides - chemical synthesis ; Amides - chemistry ; Amides - pharmacology ; BASIC BIOLOGICAL SCIENCES ; Bruton’s tyrosine kinase (BTK) ; Carbazole ; Carbazoles - chemistry ; Carbazoles - pharmacology ; Dose-Response Relationship, Drug ; Drug Design ; Humans ; Janus kinase 2 (JAK2) ; Janus Kinase 2 - antagonists & inhibitors ; Janus Kinase 2 - metabolism ; Molecular Structure ; Protein Kinase Inhibitors - chemical synthesis ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacology ; Protein-Tyrosine Kinases - antagonists & inhibitors ; Protein-Tyrosine Kinases - metabolism ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (19), p.4265-4269</ispartof><rights>2015 Elsevier Ltd</rights><rights>Copyright © 2015 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c453t-5ad3856d9ed26cf1aea27540e073e558b6caa8ed5da142cf41c9d5e6d4ac44933</citedby><cites>FETCH-LOGICAL-c453t-5ad3856d9ed26cf1aea27540e073e558b6caa8ed5da142cf41c9d5e6d4ac44933</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X15008215$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3537,27901,27902,65534</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26320619$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.osti.gov/biblio/1347758$$D View this record in Osti.gov$$Hfree_for_read</backlink></links><search><creatorcontrib>Liu, Qingjie</creatorcontrib><creatorcontrib>Batt, Douglas G.</creatorcontrib><creatorcontrib>Lippy, Jonathan S.</creatorcontrib><creatorcontrib>Surti, Neha</creatorcontrib><creatorcontrib>Tebben, Andrew J.</creatorcontrib><creatorcontrib>Muckelbauer, Jodi K.</creatorcontrib><creatorcontrib>Chen, Lin</creatorcontrib><creatorcontrib>An, Yongmi</creatorcontrib><creatorcontrib>Chang, Chiehying</creatorcontrib><creatorcontrib>Pokross, Matt</creatorcontrib><creatorcontrib>Yang, Zheng</creatorcontrib><creatorcontrib>Wang, Haiqing</creatorcontrib><creatorcontrib>Burke, James R.</creatorcontrib><creatorcontrib>Carter, Percy H.</creatorcontrib><creatorcontrib>Tino, Joseph A.</creatorcontrib><creatorcontrib>Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)</creatorcontrib><title>Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).</description><subject>60 APPLIED LIFE SCIENCES</subject><subject>Amides - chemical synthesis</subject><subject>Amides - chemistry</subject><subject>Amides - pharmacology</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>Bruton’s tyrosine kinase (BTK)</subject><subject>Carbazole</subject><subject>Carbazoles - chemistry</subject><subject>Carbazoles - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Design</subject><subject>Humans</subject><subject>Janus kinase 2 (JAK2)</subject><subject>Janus Kinase 2 - antagonists & inhibitors</subject><subject>Janus Kinase 2 - metabolism</subject><subject>Molecular Structure</subject><subject>Protein Kinase Inhibitors - chemical synthesis</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Protein-Tyrosine Kinases - antagonists & inhibitors</subject><subject>Protein-Tyrosine Kinases - metabolism</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc1u1DAUhS0EotPCC7BAFqvpIoPt2E4isekPf20lNkViZzn2TcdDYrd2ghhWLHgJXo8nwZlpWbKyffWdc-_1QegFJStKqHy9WbWD6VeMULEiVa6xR2hBueRFyYl4jBakkaSoG_7lAB2mtCGEcsL5U3TAZMmIpM0C_TqH5G481t7itPXjOj8TDh02Orb6R-hhdwvf9eAsJKwTvo1hcMn5G-z82rVuDHGnOI3TGPyfn78THrcxZALwV-d1Arw8vb483vW40H5KD2WGlxcnl-z4GXrS6T7B8_vzCH1-9_b67ENx9en9x7OTq8JwUY6F0LashbQNWCZNRzVoVglOgFQlCFG30mhdgxVWU85Mx6lprABpuTacN2V5hF7tfUManUrGjWDWJngPZlS05FUl6gwt91De826CNKq8rYG-1x7ClBStKBVc1I3MKNujJq-bInTqNrpBx62iRM0RqY2aI1JzRIpUucay6OW9_9QOYP9JHjLJwJs9APkrvjmI86TgDVgX50FtcP_z_wvY0KOI</recordid><startdate>20151001</startdate><enddate>20151001</enddate><creator>Liu, Qingjie</creator><creator>Batt, Douglas G.</creator><creator>Lippy, Jonathan S.</creator><creator>Surti, Neha</creator><creator>Tebben, Andrew J.</creator><creator>Muckelbauer, Jodi K.</creator><creator>Chen, Lin</creator><creator>An, Yongmi</creator><creator>Chang, Chiehying</creator><creator>Pokross, Matt</creator><creator>Yang, Zheng</creator><creator>Wang, Haiqing</creator><creator>Burke, James R.</creator><creator>Carter, Percy H.</creator><creator>Tino, Joseph A.</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>OTOTI</scope></search><sort><creationdate>20151001</creationdate><title>Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)</title><author>Liu, Qingjie ; Batt, Douglas G. ; Lippy, Jonathan S. ; Surti, Neha ; Tebben, Andrew J. ; Muckelbauer, Jodi K. ; Chen, Lin ; An, Yongmi ; Chang, Chiehying ; Pokross, Matt ; Yang, Zheng ; Wang, Haiqing ; Burke, James R. ; Carter, Percy H. ; Tino, Joseph A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c453t-5ad3856d9ed26cf1aea27540e073e558b6caa8ed5da142cf41c9d5e6d4ac44933</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>60 APPLIED LIFE SCIENCES</topic><topic>Amides - chemical synthesis</topic><topic>Amides - chemistry</topic><topic>Amides - pharmacology</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>Bruton’s tyrosine kinase (BTK)</topic><topic>Carbazole</topic><topic>Carbazoles - chemistry</topic><topic>Carbazoles - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Design</topic><topic>Humans</topic><topic>Janus kinase 2 (JAK2)</topic><topic>Janus Kinase 2 - antagonists & inhibitors</topic><topic>Janus Kinase 2 - metabolism</topic><topic>Molecular Structure</topic><topic>Protein Kinase Inhibitors - chemical synthesis</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Protein-Tyrosine Kinases - antagonists & inhibitors</topic><topic>Protein-Tyrosine Kinases - metabolism</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Liu, Qingjie</creatorcontrib><creatorcontrib>Batt, Douglas G.</creatorcontrib><creatorcontrib>Lippy, Jonathan S.</creatorcontrib><creatorcontrib>Surti, Neha</creatorcontrib><creatorcontrib>Tebben, Andrew J.</creatorcontrib><creatorcontrib>Muckelbauer, Jodi K.</creatorcontrib><creatorcontrib>Chen, Lin</creatorcontrib><creatorcontrib>An, Yongmi</creatorcontrib><creatorcontrib>Chang, Chiehying</creatorcontrib><creatorcontrib>Pokross, Matt</creatorcontrib><creatorcontrib>Yang, Zheng</creatorcontrib><creatorcontrib>Wang, Haiqing</creatorcontrib><creatorcontrib>Burke, James R.</creatorcontrib><creatorcontrib>Carter, Percy H.</creatorcontrib><creatorcontrib>Tino, Joseph A.</creatorcontrib><creatorcontrib>Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)</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>OSTI.GOV</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Liu, Qingjie</au><au>Batt, Douglas G.</au><au>Lippy, Jonathan S.</au><au>Surti, Neha</au><au>Tebben, Andrew J.</au><au>Muckelbauer, Jodi K.</au><au>Chen, Lin</au><au>An, Yongmi</au><au>Chang, Chiehying</au><au>Pokross, Matt</au><au>Yang, Zheng</au><au>Wang, Haiqing</au><au>Burke, James R.</au><au>Carter, Percy H.</au><au>Tino, Joseph A.</au><aucorp>Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2015-10-01</date><risdate>2015</risdate><volume>25</volume><issue>19</issue><spage>4265</spage><epage>4269</epage><pages>4265-4269</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>26320619</pmid><doi>10.1016/j.bmcl.2015.07.102</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (19), p.4265-4269 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 60 APPLIED LIFE SCIENCES Amides - chemical synthesis Amides - chemistry Amides - pharmacology BASIC BIOLOGICAL SCIENCES Bruton’s tyrosine kinase (BTK) Carbazole Carbazoles - chemistry Carbazoles - pharmacology Dose-Response Relationship, Drug Drug Design Humans Janus kinase 2 (JAK2) Janus Kinase 2 - antagonists & inhibitors Janus Kinase 2 - metabolism Molecular Structure Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - metabolism Structure-Activity Relationship |
| title | Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2) |
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