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1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1)
We have identified the N 1-benzyl- N 2-methylethane-1,2-diamine unit as a substitute for the ( S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecess...
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| Published in: | Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (23), p.6725-6732 |
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| Main Authors: | , , , , , , , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c385t-d2ddd630cb9096aa902e9f9324000c8a0e8cc5a525f9bf69f7dbe9343214714c3 |
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| cites | cdi_FETCH-LOGICAL-c385t-d2ddd630cb9096aa902e9f9324000c8a0e8cc5a525f9bf69f7dbe9343214714c3 |
| container_end_page | 6732 |
| container_issue | 23 |
| container_start_page | 6725 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 19 |
| creator | Therrien, Eric Larouche, Guillaume Manku, Sukhdev Allan, Martin Nguyen, Natalie Styhler, Sylvia Robert, Marie-France Goulet, Anne-Christine Besterman, Jeffrey M. Nguyen, Hannah Wahhab, Amal |
| description | We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.
We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved. |
| doi_str_mv | 10.1016/j.bmcl.2009.09.110 |
| format | article |
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N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.
We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2009.09.110</identifier><identifier>PMID: 19836951</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Antineoplastic agents ; Biological and medical sciences ; CARM1 inhibitors ; Co-activator associated arginine methyltransferase 1 ; Diamines - chemical synthesis ; Diamines - chemistry ; Diamines - pharmacology ; Drug Design ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - chemistry ; Enzyme Inhibitors - pharmacology ; General aspects ; Histone methyltransferase inhibitors ; Medical sciences ; Models, Molecular ; Molecular Structure ; Pharmacology. Drug treatments ; PRMT4 inhibitors ; Protein-Arginine N-Methyltransferases - antagonists & inhibitors ; Stereoisomerism ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2009-12, Vol.19 (23), p.6725-6732</ispartof><rights>2009 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c385t-d2ddd630cb9096aa902e9f9324000c8a0e8cc5a525f9bf69f7dbe9343214714c3</citedby><cites>FETCH-LOGICAL-c385t-d2ddd630cb9096aa902e9f9324000c8a0e8cc5a525f9bf69f7dbe9343214714c3</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=22153722$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19836951$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Therrien, Eric</creatorcontrib><creatorcontrib>Larouche, Guillaume</creatorcontrib><creatorcontrib>Manku, Sukhdev</creatorcontrib><creatorcontrib>Allan, Martin</creatorcontrib><creatorcontrib>Nguyen, Natalie</creatorcontrib><creatorcontrib>Styhler, Sylvia</creatorcontrib><creatorcontrib>Robert, Marie-France</creatorcontrib><creatorcontrib>Goulet, Anne-Christine</creatorcontrib><creatorcontrib>Besterman, Jeffrey M.</creatorcontrib><creatorcontrib>Nguyen, Hannah</creatorcontrib><creatorcontrib>Wahhab, Amal</creatorcontrib><title>1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1)</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.
We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.</description><subject>Antineoplastic agents</subject><subject>Biological and medical sciences</subject><subject>CARM1 inhibitors</subject><subject>Co-activator associated arginine methyltransferase 1</subject><subject>Diamines - chemical synthesis</subject><subject>Diamines - chemistry</subject><subject>Diamines - pharmacology</subject><subject>Drug Design</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>General aspects</subject><subject>Histone methyltransferase inhibitors</subject><subject>Medical sciences</subject><subject>Models, Molecular</subject><subject>Molecular Structure</subject><subject>Pharmacology. Drug treatments</subject><subject>PRMT4 inhibitors</subject><subject>Protein-Arginine N-Methyltransferases - antagonists & inhibitors</subject><subject>Stereoisomerism</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><recordid>eNp9kE2LFDEQhoMo7rj6BzxIX0QFe6xK0j0d2MsyfsKKIAriJVQnFTdDf6xJz8L-ezPMoDehoKDqeYviEeIpwhoB2ze7dT-6YS0BzLoUItwTK9StrpWG5r5YgWmh7oz-cSYe5bwDQA1aPxRnaDrVmgZX4ie-lvXbSGOcOFeUqzhdxz4uc8rVHCo31-SWeEtlULZ5dpEW9hWlX3EqkWrk5fpuWBJNOXCizBVWL7eXXz_jq8fiQaAh85NTPxff37_7tv1YX3358Gl7eVU71TVL7aX3vlXgelP-JTIg2QSjpAYA1xFw51xDjWyC6UNrwsb3bJRWEvUGtVPn4sXx7k2af-85L3aM2fEw0MTzPtuN0ihVi6qQ8ki6NOecONibFEdKdxbBHpTanT0otQeltlRRWkLPTuf3_cj-X-TksADPTwBlR0MoLlzMfzkpsVEbKQt3ceS4yLiNnGx2kSfHPiZ2i_Vz_N8ffwB6s5Nw</recordid><startdate>20091201</startdate><enddate>20091201</enddate><creator>Therrien, Eric</creator><creator>Larouche, Guillaume</creator><creator>Manku, Sukhdev</creator><creator>Allan, Martin</creator><creator>Nguyen, Natalie</creator><creator>Styhler, Sylvia</creator><creator>Robert, Marie-France</creator><creator>Goulet, Anne-Christine</creator><creator>Besterman, Jeffrey M.</creator><creator>Nguyen, Hannah</creator><creator>Wahhab, Amal</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>20091201</creationdate><title>1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1)</title><author>Therrien, Eric ; Larouche, Guillaume ; Manku, Sukhdev ; Allan, Martin ; Nguyen, Natalie ; Styhler, Sylvia ; Robert, Marie-France ; Goulet, Anne-Christine ; Besterman, Jeffrey M. ; Nguyen, Hannah ; Wahhab, Amal</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c385t-d2ddd630cb9096aa902e9f9324000c8a0e8cc5a525f9bf69f7dbe9343214714c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Antineoplastic agents</topic><topic>Biological and medical sciences</topic><topic>CARM1 inhibitors</topic><topic>Co-activator associated arginine methyltransferase 1</topic><topic>Diamines - chemical synthesis</topic><topic>Diamines - chemistry</topic><topic>Diamines - pharmacology</topic><topic>Drug Design</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General aspects</topic><topic>Histone methyltransferase inhibitors</topic><topic>Medical sciences</topic><topic>Models, Molecular</topic><topic>Molecular Structure</topic><topic>Pharmacology. Drug treatments</topic><topic>PRMT4 inhibitors</topic><topic>Protein-Arginine N-Methyltransferases - antagonists & inhibitors</topic><topic>Stereoisomerism</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Therrien, Eric</creatorcontrib><creatorcontrib>Larouche, Guillaume</creatorcontrib><creatorcontrib>Manku, Sukhdev</creatorcontrib><creatorcontrib>Allan, Martin</creatorcontrib><creatorcontrib>Nguyen, Natalie</creatorcontrib><creatorcontrib>Styhler, Sylvia</creatorcontrib><creatorcontrib>Robert, Marie-France</creatorcontrib><creatorcontrib>Goulet, Anne-Christine</creatorcontrib><creatorcontrib>Besterman, Jeffrey M.</creatorcontrib><creatorcontrib>Nguyen, Hannah</creatorcontrib><creatorcontrib>Wahhab, Amal</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>Therrien, Eric</au><au>Larouche, Guillaume</au><au>Manku, Sukhdev</au><au>Allan, Martin</au><au>Nguyen, Natalie</au><au>Styhler, Sylvia</au><au>Robert, Marie-France</au><au>Goulet, Anne-Christine</au><au>Besterman, Jeffrey M.</au><au>Nguyen, Hannah</au><au>Wahhab, Amal</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1)</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2009-12-01</date><risdate>2009</risdate><volume>19</volume><issue>23</issue><spage>6725</spage><epage>6732</epage><pages>6725-6732</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.
We have identified the
N
1-benzyl-
N
2-methylethane-1,2-diamine unit as a substitute for the (
S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19836951</pmid><doi>10.1016/j.bmcl.2009.09.110</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2009-12, Vol.19 (23), p.6725-6732 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_734123613 |
| source | ScienceDirect Freedom Collection 2022-2024 |
| subjects | Antineoplastic agents Biological and medical sciences CARM1 inhibitors Co-activator associated arginine methyltransferase 1 Diamines - chemical synthesis Diamines - chemistry Diamines - pharmacology Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Histone methyltransferase inhibitors Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments PRMT4 inhibitors Protein-Arginine N-Methyltransferases - antagonists & inhibitors Stereoisomerism Structure-Activity Relationship |
| title | 1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1) |
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