Structure-Activity Relationship Studies of Arylthiazolidine Amides as Selective Cytotoxic Agents for Melanoma
New drugs are urgently needed for improved therapy for melanoma. Materials and Methods: Ninety-one novel compounds were evaluated in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms of action for the best compound were als...
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| Veröffentlicht in: | Anticancer research 2007-03, Vol.27 (2), p.883-888 |
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| container_title | Anticancer research |
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| creator | Li, Wei Wang, Zhao Gududuru, Veeresa Zbytek, Blazej Slominski, Andrzej T Dalton, James T Miller, Duane D |
| description | New drugs are urgently needed for improved therapy for melanoma. Materials and Methods: Ninety-one novel compounds were evaluated
in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms
of action for the best compound were also investigated. Results: Three potent lead structures (serine amino alcohols, serine
amides and thiazolidines) were identified, with thiazolidines having both excellent potency and high selectivity when compared
with sorafenib, a drug used extensively in clinical trials for melanoma. Analyzing the effect of the lead compound showed
that it induced DNA degradation consistent with necrotic cell death. Conclusion: The lead structure represents a novel class
of compounds that can be further optimized for potential drug to treat advanced melanoma. |
| format | Article |
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in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms
of action for the best compound were also investigated. Results: Three potent lead structures (serine amino alcohols, serine
amides and thiazolidines) were identified, with thiazolidines having both excellent potency and high selectivity when compared
with sorafenib, a drug used extensively in clinical trials for melanoma. Analyzing the effect of the lead compound showed
that it induced DNA degradation consistent with necrotic cell death. Conclusion: The lead structure represents a novel class
of compounds that can be further optimized for potential drug to treat advanced melanoma.</description><identifier>ISSN: 0250-7005</identifier><identifier>EISSN: 1791-7530</identifier><identifier>PMID: 17465215</identifier><language>eng</language><publisher>Attiki: International Institute of Anticancer Research</publisher><subject>Amides - chemistry ; Amides - pharmacology ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Benzenesulfonates - pharmacology ; Biological and medical sciences ; Cell Death - drug effects ; Cell Growth Processes - drug effects ; Cell Line, Tumor ; Dermatology ; Humans ; Inhibitory Concentration 50 ; Medical sciences ; Melanoma - drug therapy ; Melanoma - pathology ; Necrosis ; Niacinamide - analogs & derivatives ; Phenylurea Compounds ; Pyridines - pharmacology ; Structure-Activity Relationship ; Thiazolidines - chemistry ; Thiazolidines - pharmacology ; Tumors ; Tumors of the skin and soft tissue. Premalignant lesions</subject><ispartof>Anticancer research, 2007-03, Vol.27 (2), p.883-888</ispartof><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18657600$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17465215$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Wei</creatorcontrib><creatorcontrib>Wang, Zhao</creatorcontrib><creatorcontrib>Gududuru, Veeresa</creatorcontrib><creatorcontrib>Zbytek, Blazej</creatorcontrib><creatorcontrib>Slominski, Andrzej T</creatorcontrib><creatorcontrib>Dalton, James T</creatorcontrib><creatorcontrib>Miller, Duane D</creatorcontrib><title>Structure-Activity Relationship Studies of Arylthiazolidine Amides as Selective Cytotoxic Agents for Melanoma</title><title>Anticancer research</title><addtitle>Anticancer Res</addtitle><description>New drugs are urgently needed for improved therapy for melanoma. Materials and Methods: Ninety-one novel compounds were evaluated
in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms
of action for the best compound were also investigated. Results: Three potent lead structures (serine amino alcohols, serine
amides and thiazolidines) were identified, with thiazolidines having both excellent potency and high selectivity when compared
with sorafenib, a drug used extensively in clinical trials for melanoma. Analyzing the effect of the lead compound showed
that it induced DNA degradation consistent with necrotic cell death. Conclusion: The lead structure represents a novel class
of compounds that can be further optimized for potential drug to treat advanced melanoma.</description><subject>Amides - chemistry</subject><subject>Amides - pharmacology</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Benzenesulfonates - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Death - drug effects</subject><subject>Cell Growth Processes - drug effects</subject><subject>Cell Line, Tumor</subject><subject>Dermatology</subject><subject>Humans</subject><subject>Inhibitory Concentration 50</subject><subject>Medical sciences</subject><subject>Melanoma - drug therapy</subject><subject>Melanoma - pathology</subject><subject>Necrosis</subject><subject>Niacinamide - analogs & derivatives</subject><subject>Phenylurea Compounds</subject><subject>Pyridines - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Thiazolidines - chemistry</subject><subject>Thiazolidines - pharmacology</subject><subject>Tumors</subject><subject>Tumors of the skin and soft tissue. Premalignant lesions</subject><issn>0250-7005</issn><issn>1791-7530</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFj1FLwzAUhYMobk7_guRBHwtJ0yTtYxnqhIng9Llkzc0aSduRpGr99VY28ek-nO98nHuC5lQWNJGckVM0JykniSSEz9BFCO-ECFHk7BzNqMwETymfo3YT_VDHwUNS1tF-2DjiF3Aq2r4Ljd3jTRy0hYB7g0s_uthY9d07q20HuGytniIV8AYc_NYBL8fYx_7L1rjcQRcDNr3HT5Ox61t1ic6McgGujneB3u7vXperZP388Lgs10mTijwmwDMqtC70tJID0UTnihWK1IUm1GxFxriWFKTJuObADGQAmTDSMKrTTFG2QNcH737YtqCrvbet8mP19_cE3B4BFWrljFddbcM_lwsuBSETd3PgGrtrPq2HKrTKuUnLKuVTWaVVnjP2Axx9cQY</recordid><startdate>20070301</startdate><enddate>20070301</enddate><creator>Li, Wei</creator><creator>Wang, Zhao</creator><creator>Gududuru, Veeresa</creator><creator>Zbytek, Blazej</creator><creator>Slominski, Andrzej T</creator><creator>Dalton, James T</creator><creator>Miller, Duane D</creator><general>International Institute of Anticancer Research</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>20070301</creationdate><title>Structure-Activity Relationship Studies of Arylthiazolidine Amides as Selective Cytotoxic Agents for Melanoma</title><author>Li, Wei ; Wang, Zhao ; Gududuru, Veeresa ; Zbytek, Blazej ; Slominski, Andrzej T ; Dalton, James T ; Miller, Duane D</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-h268t-e5416dd9d4655e0d0d8a39a0c9d01fb6435d71e7f45d5e3fe4ee46f7f31d24a13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Amides - chemistry</topic><topic>Amides - pharmacology</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Benzenesulfonates - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Death - drug effects</topic><topic>Cell Growth Processes - drug effects</topic><topic>Cell Line, Tumor</topic><topic>Dermatology</topic><topic>Humans</topic><topic>Inhibitory Concentration 50</topic><topic>Medical sciences</topic><topic>Melanoma - drug therapy</topic><topic>Melanoma - pathology</topic><topic>Necrosis</topic><topic>Niacinamide - analogs & derivatives</topic><topic>Phenylurea Compounds</topic><topic>Pyridines - pharmacology</topic><topic>Structure-Activity Relationship</topic><topic>Thiazolidines - chemistry</topic><topic>Thiazolidines - pharmacology</topic><topic>Tumors</topic><topic>Tumors of the skin and soft tissue. Premalignant lesions</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Wei</creatorcontrib><creatorcontrib>Wang, Zhao</creatorcontrib><creatorcontrib>Gududuru, Veeresa</creatorcontrib><creatorcontrib>Zbytek, Blazej</creatorcontrib><creatorcontrib>Slominski, Andrzej T</creatorcontrib><creatorcontrib>Dalton, James T</creatorcontrib><creatorcontrib>Miller, Duane D</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Anticancer research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Wei</au><au>Wang, Zhao</au><au>Gududuru, Veeresa</au><au>Zbytek, Blazej</au><au>Slominski, Andrzej T</au><au>Dalton, James T</au><au>Miller, Duane D</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure-Activity Relationship Studies of Arylthiazolidine Amides as Selective Cytotoxic Agents for Melanoma</atitle><jtitle>Anticancer research</jtitle><addtitle>Anticancer Res</addtitle><date>2007-03-01</date><risdate>2007</risdate><volume>27</volume><issue>2</issue><spage>883</spage><epage>888</epage><pages>883-888</pages><issn>0250-7005</issn><eissn>1791-7530</eissn><abstract>New drugs are urgently needed for improved therapy for melanoma. Materials and Methods: Ninety-one novel compounds were evaluated
in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms
of action for the best compound were also investigated. Results: Three potent lead structures (serine amino alcohols, serine
amides and thiazolidines) were identified, with thiazolidines having both excellent potency and high selectivity when compared
with sorafenib, a drug used extensively in clinical trials for melanoma. Analyzing the effect of the lead compound showed
that it induced DNA degradation consistent with necrotic cell death. Conclusion: The lead structure represents a novel class
of compounds that can be further optimized for potential drug to treat advanced melanoma.</abstract><cop>Attiki</cop><pub>International Institute of Anticancer Research</pub><pmid>17465215</pmid><tpages>6</tpages></addata></record> |
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| ispartof | Anticancer research, 2007-03, Vol.27 (2), p.883-888 |
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| language | eng |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | Amides - chemistry Amides - pharmacology Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzenesulfonates - pharmacology Biological and medical sciences Cell Death - drug effects Cell Growth Processes - drug effects Cell Line, Tumor Dermatology Humans Inhibitory Concentration 50 Medical sciences Melanoma - drug therapy Melanoma - pathology Necrosis Niacinamide - analogs & derivatives Phenylurea Compounds Pyridines - pharmacology Structure-Activity Relationship Thiazolidines - chemistry Thiazolidines - pharmacology Tumors Tumors of the skin and soft tissue. Premalignant lesions |
| title | Structure-Activity Relationship Studies of Arylthiazolidine Amides as Selective Cytotoxic Agents for Melanoma |
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