The development of benzimidazoles as selective rho kinase inhibitors
Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC 50
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1939-1943 |
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| container_end_page | 1943 |
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| container_issue | 6 |
| container_start_page | 1939 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 20 |
| creator | Sessions, E. Hampton Smolinski, Michael Wang, Bo Frackowiak, Bozena Chowdhury, Sarwat Yin, Yan Chen, Yen Ting Ruiz, Claudia Lin, Li Pocas, Jennifer Schröter, Thomas Cameron, Michael D. LoGrasso, Philip Feng, Yangbo Bannister, Thomas D. |
| description | Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC
50 |
| doi_str_mv | 10.1016/j.bmcl.2010.01.124 |
| format | Article |
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nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.01.124</identifier><identifier>PMID: 20167489</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Benzimidazole ; Benzimidazoles - pharmacology ; Biological and medical sciences ; Chroman ; Eye ; Glaucoma ; Medical sciences ; Pharmacology. Drug treatments ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacology ; Rho Kinase ; rho-Associated Kinases - antagonists & inhibitors ; ROCK</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (6), p.1939-1943</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-c417t-e6526bb0e41e2dc64c33d92e67a320c25fea40301dc8623e9340c2d8423bb6343</citedby><cites>FETCH-LOGICAL-c417t-e6526bb0e41e2dc64c33d92e67a320c25fea40301dc8623e9340c2d8423bb6343</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.2010.01.124$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27907,27908,45978</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22824827$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20167489$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sessions, E. Hampton</creatorcontrib><creatorcontrib>Smolinski, Michael</creatorcontrib><creatorcontrib>Wang, Bo</creatorcontrib><creatorcontrib>Frackowiak, Bozena</creatorcontrib><creatorcontrib>Chowdhury, Sarwat</creatorcontrib><creatorcontrib>Yin, Yan</creatorcontrib><creatorcontrib>Chen, Yen Ting</creatorcontrib><creatorcontrib>Ruiz, Claudia</creatorcontrib><creatorcontrib>Lin, Li</creatorcontrib><creatorcontrib>Pocas, Jennifer</creatorcontrib><creatorcontrib>Schröter, Thomas</creatorcontrib><creatorcontrib>Cameron, Michael D.</creatorcontrib><creatorcontrib>LoGrasso, Philip</creatorcontrib><creatorcontrib>Feng, Yangbo</creatorcontrib><creatorcontrib>Bannister, Thomas D.</creatorcontrib><title>The development of benzimidazoles as selective rho kinase inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC
50
<10
nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).</description><subject>Benzimidazole</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Chroman</subject><subject>Eye</subject><subject>Glaucoma</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Rho Kinase</subject><subject>rho-Associated Kinases - antagonists & inhibitors</subject><subject>ROCK</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1r3DAQhkVJaDZp_0APxZeQkzcjaVa2oZeSbwjkkkBvQpbGrLa2tZW8C82vj5bdNrf2NDA873w8jH3hMOfA1eVq3g62nwvIDeBzLvADm3FUWEqExRGbQaOgrBv8ccJOU1oBcATEj-wkR1SFdTNj189LKhxtqQ_rgcapCF3R0vjqB-_Ma-gpFSYViXqyk99SEZeh-OlHk6jw49K3fgoxfWLHnekTfT7UM_Zye_N8dV8-Pt09XH1_LC3yaipJLYRqWyDkJJxVaKV0jSBVGSnAikVHBkECd7ZWQlKT37DC1Shk2yqJ8oxd7OeuY_i1oTTpwSdLfW9GCpukK1R8ISts_k9KWUElVJVJsSdtDClF6vQ6-sHE35qD3mnWK73TrHeaNXCdNefQ18P4TTuQ-xv54zUD5wfAJGv6LprR-vTOiVpgLXbbv-05ytq2nqJO1tNoyfmYjWsX_L_ueAO3WZo6</recordid><startdate>20100315</startdate><enddate>20100315</enddate><creator>Sessions, E. Hampton</creator><creator>Smolinski, Michael</creator><creator>Wang, Bo</creator><creator>Frackowiak, Bozena</creator><creator>Chowdhury, Sarwat</creator><creator>Yin, Yan</creator><creator>Chen, Yen Ting</creator><creator>Ruiz, Claudia</creator><creator>Lin, Li</creator><creator>Pocas, Jennifer</creator><creator>Schröter, Thomas</creator><creator>Cameron, Michael D.</creator><creator>LoGrasso, Philip</creator><creator>Feng, Yangbo</creator><creator>Bannister, Thomas D.</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>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20100315</creationdate><title>The development of benzimidazoles as selective rho kinase inhibitors</title><author>Sessions, E. Hampton ; Smolinski, Michael ; Wang, Bo ; Frackowiak, Bozena ; Chowdhury, Sarwat ; Yin, Yan ; Chen, Yen Ting ; Ruiz, Claudia ; Lin, Li ; Pocas, Jennifer ; Schröter, Thomas ; Cameron, Michael D. ; LoGrasso, Philip ; Feng, Yangbo ; Bannister, Thomas D.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-e6526bb0e41e2dc64c33d92e67a320c25fea40301dc8623e9340c2d8423bb6343</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Benzimidazole</topic><topic>Benzimidazoles - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Chroman</topic><topic>Eye</topic><topic>Glaucoma</topic><topic>Medical sciences</topic><topic>Pharmacology. 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Hampton</au><au>Smolinski, Michael</au><au>Wang, Bo</au><au>Frackowiak, Bozena</au><au>Chowdhury, Sarwat</au><au>Yin, Yan</au><au>Chen, Yen Ting</au><au>Ruiz, Claudia</au><au>Lin, Li</au><au>Pocas, Jennifer</au><au>Schröter, Thomas</au><au>Cameron, Michael D.</au><au>LoGrasso, Philip</au><au>Feng, Yangbo</au><au>Bannister, Thomas D.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The development of benzimidazoles as selective rho kinase inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-03-15</date><risdate>2010</risdate><volume>20</volume><issue>6</issue><spage>1939</spage><epage>1943</epage><pages>1939-1943</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. 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50
<10
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| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (6), p.1939-1943 |
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| language | eng |
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| source | Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE |
| subjects | Benzimidazole Benzimidazoles - pharmacology Biological and medical sciences Chroman Eye Glaucoma Medical sciences Pharmacology. Drug treatments Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Rho Kinase rho-Associated Kinases - antagonists & inhibitors ROCK |
| title | The development of benzimidazoles as selective rho kinase inhibitors |
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