Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines
[Display omitted] Sigma Receptor (SR) modulators are involved in different signal transduction pathways, representing important pharmacological/therapeutic tools in several pathological conditions, such as neurodegenerative diseases and cancers. To this purpose, numerous compounds have been develope...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2017-01, Vol.25 (1), p.11-19 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Rossi, Daniela Rui, Marta Di Giacomo, Marcello Schepmann, Dirk Wünsch, Bernhard Monteleone, Stefania Liedl, Klaus R. Collina, Simona |
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Sigma Receptor (SR) modulators are involved in different signal transduction pathways, representing important pharmacological/therapeutic tools in several pathological conditions, such as neurodegenerative diseases and cancers. To this purpose, numerous compounds have been developed in order to target selectively one of the two subtypes (S1R and S2R) as chemotherapeutic agent. However, experiments have also shown that ligands which are able to bind both SR subtypes can be useful for the diagnosis and/or the treatment of cancers. Therefore, the discovery of compounds with good affinity towards both S1R and S2R (‘pan-modulators’) is also of great interest and still represents a challenge up to now. For this reason, we synthesized novel arylalkylamines with the aim to obtain compounds with S1R and S2R affinity in the nM range and, by modeling quantitative structure–activity relationships (QSARs), we identified the essential structural features to obtain promising pan-compounds. |
| doi_str_mv | 10.1016/j.bmc.2016.10.005 |
| format | Article |
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Sigma Receptor (SR) modulators are involved in different signal transduction pathways, representing important pharmacological/therapeutic tools in several pathological conditions, such as neurodegenerative diseases and cancers. To this purpose, numerous compounds have been developed in order to target selectively one of the two subtypes (S1R and S2R) as chemotherapeutic agent. However, experiments have also shown that ligands which are able to bind both SR subtypes can be useful for the diagnosis and/or the treatment of cancers. Therefore, the discovery of compounds with good affinity towards both S1R and S2R (‘pan-modulators’) is also of great interest and still represents a challenge up to now. For this reason, we synthesized novel arylalkylamines with the aim to obtain compounds with S1R and S2R affinity in the nM range and, by modeling quantitative structure–activity relationships (QSARs), we identified the essential structural features to obtain promising pan-compounds.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2016.10.005</identifier><identifier>PMID: 27838169</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Alkylation ; Amination ; Amines - chemistry ; Amines - pharmacology ; Animals ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Arylalkylamine ; Drug Discovery ; Guinea Pigs ; Humans ; Hydrocarbons, Aromatic - chemistry ; Hydrocarbons, Aromatic - pharmacology ; Ligands ; Neoplasms - diagnosis ; Neoplasms - drug therapy ; Neoplasms - metabolism ; Pan-affinity ; QSAR ; Quantitative Structure-Activity Relationship ; Receptors, sigma - agonists ; Receptors, sigma - antagonists & inhibitors ; Receptors, sigma - metabolism ; Sigma receptors ; Sigma-1 Receptor</subject><ispartof>Bioorganic & medicinal chemistry, 2017-01, Vol.25 (1), p.11-19</ispartof><rights>2016 Elsevier Ltd</rights><rights>Copyright © 2016 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c353t-406d99ee7a9820b1041937032b9af622a899e1651d67fac853ed8507332a07103</citedby><cites>FETCH-LOGICAL-c353t-406d99ee7a9820b1041937032b9af622a899e1651d67fac853ed8507332a07103</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmc.2016.10.005$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27838169$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Rossi, Daniela</creatorcontrib><creatorcontrib>Rui, Marta</creatorcontrib><creatorcontrib>Di Giacomo, Marcello</creatorcontrib><creatorcontrib>Schepmann, Dirk</creatorcontrib><creatorcontrib>Wünsch, Bernhard</creatorcontrib><creatorcontrib>Monteleone, Stefania</creatorcontrib><creatorcontrib>Liedl, Klaus R.</creatorcontrib><creatorcontrib>Collina, Simona</creatorcontrib><title>Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
Sigma Receptor (SR) modulators are involved in different signal transduction pathways, representing important pharmacological/therapeutic tools in several pathological conditions, such as neurodegenerative diseases and cancers. To this purpose, numerous compounds have been developed in order to target selectively one of the two subtypes (S1R and S2R) as chemotherapeutic agent. However, experiments have also shown that ligands which are able to bind both SR subtypes can be useful for the diagnosis and/or the treatment of cancers. Therefore, the discovery of compounds with good affinity towards both S1R and S2R (‘pan-modulators’) is also of great interest and still represents a challenge up to now. For this reason, we synthesized novel arylalkylamines with the aim to obtain compounds with S1R and S2R affinity in the nM range and, by modeling quantitative structure–activity relationships (QSARs), we identified the essential structural features to obtain promising pan-compounds.</description><subject>Alkylation</subject><subject>Amination</subject><subject>Amines - chemistry</subject><subject>Amines - pharmacology</subject><subject>Animals</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Arylalkylamine</subject><subject>Drug Discovery</subject><subject>Guinea Pigs</subject><subject>Humans</subject><subject>Hydrocarbons, Aromatic - chemistry</subject><subject>Hydrocarbons, Aromatic - pharmacology</subject><subject>Ligands</subject><subject>Neoplasms - diagnosis</subject><subject>Neoplasms - drug therapy</subject><subject>Neoplasms - metabolism</subject><subject>Pan-affinity</subject><subject>QSAR</subject><subject>Quantitative Structure-Activity Relationship</subject><subject>Receptors, sigma - agonists</subject><subject>Receptors, sigma - antagonists & inhibitors</subject><subject>Receptors, sigma - metabolism</subject><subject>Sigma receptors</subject><subject>Sigma-1 Receptor</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtPLCEQhYnR6Pj4AW4MSzfdFtBNQ1wZc30kJiY-loYwTbVh7KbnQo83_nuZzHiXbqAKzjmp-gg5ZVAyYPJiUc6HtuS5zH0JUO-QGatkVQih2S6ZgZaqAKXlATlMaQEAvNJsnxzwRgnFpJ6Rt1vrgw_v1Ae6tKGwXZf76YtO4z8bXaLJvw-WMmqD29acRmxxOY0xlfT56ommaeU8JjoGauNXb_uPfAw-YDome53tE55s7yPyevPn5fqueHi8vb--eihaUYupqEA6rREbqxWHOYOKadGA4HNtO8m5VfmXyZo52XS2VbVAp2pohOAWGgbiiJxvcpdx_LvCNJnBpxb73gYcV8kwlYHkWK2ylG2kbRxTitiZZfRDntswMGuqZmEyVbOmun7KVLPnbBu_mg_o_jt-MGbB5UaAeclPj9Gk1mNo0fnMajJu9L_EfwMqtYXr</recordid><startdate>20170101</startdate><enddate>20170101</enddate><creator>Rossi, Daniela</creator><creator>Rui, Marta</creator><creator>Di Giacomo, Marcello</creator><creator>Schepmann, Dirk</creator><creator>Wünsch, Bernhard</creator><creator>Monteleone, Stefania</creator><creator>Liedl, Klaus R.</creator><creator>Collina, Simona</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></search><sort><creationdate>20170101</creationdate><title>Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines</title><author>Rossi, Daniela ; Rui, Marta ; Di Giacomo, Marcello ; Schepmann, Dirk ; Wünsch, Bernhard ; Monteleone, Stefania ; Liedl, Klaus R. ; Collina, Simona</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c353t-406d99ee7a9820b1041937032b9af622a899e1651d67fac853ed8507332a07103</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Alkylation</topic><topic>Amination</topic><topic>Amines - chemistry</topic><topic>Amines - pharmacology</topic><topic>Animals</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Arylalkylamine</topic><topic>Drug Discovery</topic><topic>Guinea Pigs</topic><topic>Humans</topic><topic>Hydrocarbons, Aromatic - chemistry</topic><topic>Hydrocarbons, Aromatic - pharmacology</topic><topic>Ligands</topic><topic>Neoplasms - diagnosis</topic><topic>Neoplasms - drug therapy</topic><topic>Neoplasms - metabolism</topic><topic>Pan-affinity</topic><topic>QSAR</topic><topic>Quantitative Structure-Activity Relationship</topic><topic>Receptors, sigma - agonists</topic><topic>Receptors, sigma - antagonists & inhibitors</topic><topic>Receptors, sigma - metabolism</topic><topic>Sigma receptors</topic><topic>Sigma-1 Receptor</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rossi, Daniela</creatorcontrib><creatorcontrib>Rui, Marta</creatorcontrib><creatorcontrib>Di Giacomo, Marcello</creatorcontrib><creatorcontrib>Schepmann, Dirk</creatorcontrib><creatorcontrib>Wünsch, Bernhard</creatorcontrib><creatorcontrib>Monteleone, Stefania</creatorcontrib><creatorcontrib>Liedl, Klaus R.</creatorcontrib><creatorcontrib>Collina, Simona</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><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Rossi, Daniela</au><au>Rui, Marta</au><au>Di Giacomo, Marcello</au><au>Schepmann, Dirk</au><au>Wünsch, Bernhard</au><au>Monteleone, Stefania</au><au>Liedl, Klaus R.</au><au>Collina, Simona</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2017-01-01</date><risdate>2017</risdate><volume>25</volume><issue>1</issue><spage>11</spage><epage>19</epage><pages>11-19</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
Sigma Receptor (SR) modulators are involved in different signal transduction pathways, representing important pharmacological/therapeutic tools in several pathological conditions, such as neurodegenerative diseases and cancers. To this purpose, numerous compounds have been developed in order to target selectively one of the two subtypes (S1R and S2R) as chemotherapeutic agent. However, experiments have also shown that ligands which are able to bind both SR subtypes can be useful for the diagnosis and/or the treatment of cancers. Therefore, the discovery of compounds with good affinity towards both S1R and S2R (‘pan-modulators’) is also of great interest and still represents a challenge up to now. For this reason, we synthesized novel arylalkylamines with the aim to obtain compounds with S1R and S2R affinity in the nM range and, by modeling quantitative structure–activity relationships (QSARs), we identified the essential structural features to obtain promising pan-compounds.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>27838169</pmid><doi>10.1016/j.bmc.2016.10.005</doi><tpages>9</tpages></addata></record> |
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| subjects | Alkylation Amination Amines - chemistry Amines - pharmacology Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Arylalkylamine Drug Discovery Guinea Pigs Humans Hydrocarbons, Aromatic - chemistry Hydrocarbons, Aromatic - pharmacology Ligands Neoplasms - diagnosis Neoplasms - drug therapy Neoplasms - metabolism Pan-affinity QSAR Quantitative Structure-Activity Relationship Receptors, sigma - agonists Receptors, sigma - antagonists & inhibitors Receptors, sigma - metabolism Sigma receptors Sigma-1 Receptor |
| title | Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines |
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