Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds
Four new ethylnitrosourea derivatives of substituted naphthalimides 3a-d have been synthesized from the respective N-(2-ethylamino) naphthalimides. Their chemical alkylating activity compared with the clinical drug CCNU and an experimental compound Mitonafide indicated that they possess lower alkyla...
Gespeichert in:
| Veröffentlicht in: | Acta Poloniae pharmaceutica 2007-01, Vol.64 (1), p.27 |
|---|---|
| Hauptverfasser: | , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | |
|---|---|
| container_issue | 1 |
| container_start_page | 27 |
| container_title | Acta Poloniae pharmaceutica |
| container_volume | 64 |
| creator | Pain, Anindita Samanta, Suva Dutta, Sushanta Saxena, Ajit K Shanmugavel, Mutiah Sharma, Madhunika Qazi, Gulam N Sanyal, Utpal |
| description | Four new ethylnitrosourea derivatives of substituted naphthalimides 3a-d have been synthesized from the respective N-(2-ethylamino) naphthalimides. Their chemical alkylating activity compared with the clinical drug CCNU and an experimental compound Mitonafide indicated that they possess lower alkylating activity than CCNU and comparable activity with the latter. Their anti-tumor efficacies were assessed in vivo in two murine ascites tumors namely Sarcoma-180 (S-180) and Ehrlich ascites carcinoma (EAC) by measuring the increase in median survival times (MST) of drug treated (T) over untreated control (C) mice. CCNU and Mitonafide were used as positive controls for comparison. The representative compound 3a has displayed marginal anti-tumoral activity in these tumors. Three compounds were further screened in vitro in 4 different human tumor cell lines but no significant activity was observed in those lines. These compounds moderately inhibit the synthesis of DNA and RNA in S-180 tumor cells. |
| format | Article |
| fullrecord | <record><control><sourceid>pubmed</sourceid><recordid>TN_cdi_pubmed_primary_17665847</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>17665847</sourcerecordid><originalsourceid>FETCH-LOGICAL-p124t-b530bb5407843785701ce434573d5f26c45c74dce70f98764b7bc550236f36aa3</originalsourceid><addsrcrecordid>eNo1z8tqwzAUBFAtWpqQ5heKfsAgRY_rLEvoCwJdpF2Hq4exii0ZSyr475vQdjXMLA7MDVkzxnijWwErss3561KZkrDn_I6sOGitWglrYk9LLL3PIVOMjvpvHCqWkCJNHfWlX4YYypxyqrPHfB1zNbmEUot3NOLUlx6HMAbnL8IVKcFitH6mNo1TqtHle3Lb4ZD99i835PP56ePw2hzfX94Oj8dm4jtZGqMEM0ZJBq0U0Cpg3HoppALhVLfTVioL0lkPrNu3oKUBY5ViO6E7oRHFhjz8ulM1o3fnaQ4jzsv5_634ATIFUsk</addsrcrecordid><sourcetype>Index Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds</title><source>MEDLINE</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><creator>Pain, Anindita ; Samanta, Suva ; Dutta, Sushanta ; Saxena, Ajit K ; Shanmugavel, Mutiah ; Sharma, Madhunika ; Qazi, Gulam N ; Sanyal, Utpal</creator><creatorcontrib>Pain, Anindita ; Samanta, Suva ; Dutta, Sushanta ; Saxena, Ajit K ; Shanmugavel, Mutiah ; Sharma, Madhunika ; Qazi, Gulam N ; Sanyal, Utpal</creatorcontrib><description>Four new ethylnitrosourea derivatives of substituted naphthalimides 3a-d have been synthesized from the respective N-(2-ethylamino) naphthalimides. Their chemical alkylating activity compared with the clinical drug CCNU and an experimental compound Mitonafide indicated that they possess lower alkylating activity than CCNU and comparable activity with the latter. Their anti-tumor efficacies were assessed in vivo in two murine ascites tumors namely Sarcoma-180 (S-180) and Ehrlich ascites carcinoma (EAC) by measuring the increase in median survival times (MST) of drug treated (T) over untreated control (C) mice. CCNU and Mitonafide were used as positive controls for comparison. The representative compound 3a has displayed marginal anti-tumoral activity in these tumors. Three compounds were further screened in vitro in 4 different human tumor cell lines but no significant activity was observed in those lines. These compounds moderately inhibit the synthesis of DNA and RNA in S-180 tumor cells.</description><identifier>ISSN: 0001-6837</identifier><identifier>PMID: 17665847</identifier><language>eng</language><publisher>Poland</publisher><subject>Animals ; Antineoplastic Agents, Alkylating - chemical synthesis ; Antineoplastic Agents, Alkylating - chemistry ; Antineoplastic Agents, Alkylating - pharmacology ; Carcinoma, Ehrlich Tumor - drug therapy ; Cell Line, Tumor ; DNA - biosynthesis ; DNA - drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Imides - pharmacology ; Isoquinolines - pharmacology ; Lomustine - pharmacology ; Mice ; Naphthalimides - chemical synthesis ; Naphthalimides - chemistry ; Naphthalimides - pharmacology ; Nitrosourea Compounds - administration & dosage ; Nitrosourea Compounds - chemical synthesis ; Nitrosourea Compounds - chemistry ; Nitrosourea Compounds - pharmacology ; RNA - biosynthesis ; RNA - drug effects ; Sarcoma 180 - drug therapy ; Structure-Activity Relationship</subject><ispartof>Acta Poloniae pharmaceutica, 2007-01, Vol.64 (1), p.27</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17665847$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Pain, Anindita</creatorcontrib><creatorcontrib>Samanta, Suva</creatorcontrib><creatorcontrib>Dutta, Sushanta</creatorcontrib><creatorcontrib>Saxena, Ajit K</creatorcontrib><creatorcontrib>Shanmugavel, Mutiah</creatorcontrib><creatorcontrib>Sharma, Madhunika</creatorcontrib><creatorcontrib>Qazi, Gulam N</creatorcontrib><creatorcontrib>Sanyal, Utpal</creatorcontrib><title>Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds</title><title>Acta Poloniae pharmaceutica</title><addtitle>Acta Pol Pharm</addtitle><description>Four new ethylnitrosourea derivatives of substituted naphthalimides 3a-d have been synthesized from the respective N-(2-ethylamino) naphthalimides. Their chemical alkylating activity compared with the clinical drug CCNU and an experimental compound Mitonafide indicated that they possess lower alkylating activity than CCNU and comparable activity with the latter. Their anti-tumor efficacies were assessed in vivo in two murine ascites tumors namely Sarcoma-180 (S-180) and Ehrlich ascites carcinoma (EAC) by measuring the increase in median survival times (MST) of drug treated (T) over untreated control (C) mice. CCNU and Mitonafide were used as positive controls for comparison. The representative compound 3a has displayed marginal anti-tumoral activity in these tumors. Three compounds were further screened in vitro in 4 different human tumor cell lines but no significant activity was observed in those lines. These compounds moderately inhibit the synthesis of DNA and RNA in S-180 tumor cells.</description><subject>Animals</subject><subject>Antineoplastic Agents, Alkylating - chemical synthesis</subject><subject>Antineoplastic Agents, Alkylating - chemistry</subject><subject>Antineoplastic Agents, Alkylating - pharmacology</subject><subject>Carcinoma, Ehrlich Tumor - drug therapy</subject><subject>Cell Line, Tumor</subject><subject>DNA - biosynthesis</subject><subject>DNA - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Humans</subject><subject>Imides - pharmacology</subject><subject>Isoquinolines - pharmacology</subject><subject>Lomustine - pharmacology</subject><subject>Mice</subject><subject>Naphthalimides - chemical synthesis</subject><subject>Naphthalimides - chemistry</subject><subject>Naphthalimides - pharmacology</subject><subject>Nitrosourea Compounds - administration & dosage</subject><subject>Nitrosourea Compounds - chemical synthesis</subject><subject>Nitrosourea Compounds - chemistry</subject><subject>Nitrosourea Compounds - pharmacology</subject><subject>RNA - biosynthesis</subject><subject>RNA - drug effects</subject><subject>Sarcoma 180 - drug therapy</subject><subject>Structure-Activity Relationship</subject><issn>0001-6837</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1z8tqwzAUBFAtWpqQ5heKfsAgRY_rLEvoCwJdpF2Hq4exii0ZSyr475vQdjXMLA7MDVkzxnijWwErss3561KZkrDn_I6sOGitWglrYk9LLL3PIVOMjvpvHCqWkCJNHfWlX4YYypxyqrPHfB1zNbmEUot3NOLUlx6HMAbnL8IVKcFitH6mNo1TqtHle3Lb4ZD99i835PP56ePw2hzfX94Oj8dm4jtZGqMEM0ZJBq0U0Cpg3HoppALhVLfTVioL0lkPrNu3oKUBY5ViO6E7oRHFhjz8ulM1o3fnaQ4jzsv5_634ATIFUsk</recordid><startdate>200701</startdate><enddate>200701</enddate><creator>Pain, Anindita</creator><creator>Samanta, Suva</creator><creator>Dutta, Sushanta</creator><creator>Saxena, Ajit K</creator><creator>Shanmugavel, Mutiah</creator><creator>Sharma, Madhunika</creator><creator>Qazi, Gulam N</creator><creator>Sanyal, Utpal</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>200701</creationdate><title>Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds</title><author>Pain, Anindita ; Samanta, Suva ; Dutta, Sushanta ; Saxena, Ajit K ; Shanmugavel, Mutiah ; Sharma, Madhunika ; Qazi, Gulam N ; Sanyal, Utpal</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p124t-b530bb5407843785701ce434573d5f26c45c74dce70f98764b7bc550236f36aa3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Animals</topic><topic>Antineoplastic Agents, Alkylating - chemical synthesis</topic><topic>Antineoplastic Agents, Alkylating - chemistry</topic><topic>Antineoplastic Agents, Alkylating - pharmacology</topic><topic>Carcinoma, Ehrlich Tumor - drug therapy</topic><topic>Cell Line, Tumor</topic><topic>DNA - biosynthesis</topic><topic>DNA - drug effects</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Humans</topic><topic>Imides - pharmacology</topic><topic>Isoquinolines - pharmacology</topic><topic>Lomustine - pharmacology</topic><topic>Mice</topic><topic>Naphthalimides - chemical synthesis</topic><topic>Naphthalimides - chemistry</topic><topic>Naphthalimides - pharmacology</topic><topic>Nitrosourea Compounds - administration & dosage</topic><topic>Nitrosourea Compounds - chemical synthesis</topic><topic>Nitrosourea Compounds - chemistry</topic><topic>Nitrosourea Compounds - pharmacology</topic><topic>RNA - biosynthesis</topic><topic>RNA - drug effects</topic><topic>Sarcoma 180 - drug therapy</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pain, Anindita</creatorcontrib><creatorcontrib>Samanta, Suva</creatorcontrib><creatorcontrib>Dutta, Sushanta</creatorcontrib><creatorcontrib>Saxena, Ajit K</creatorcontrib><creatorcontrib>Shanmugavel, Mutiah</creatorcontrib><creatorcontrib>Sharma, Madhunika</creatorcontrib><creatorcontrib>Qazi, Gulam N</creatorcontrib><creatorcontrib>Sanyal, Utpal</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Acta Poloniae pharmaceutica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pain, Anindita</au><au>Samanta, Suva</au><au>Dutta, Sushanta</au><au>Saxena, Ajit K</au><au>Shanmugavel, Mutiah</au><au>Sharma, Madhunika</au><au>Qazi, Gulam N</au><au>Sanyal, Utpal</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds</atitle><jtitle>Acta Poloniae pharmaceutica</jtitle><addtitle>Acta Pol Pharm</addtitle><date>2007-01</date><risdate>2007</risdate><volume>64</volume><issue>1</issue><spage>27</spage><pages>27-</pages><issn>0001-6837</issn><abstract>Four new ethylnitrosourea derivatives of substituted naphthalimides 3a-d have been synthesized from the respective N-(2-ethylamino) naphthalimides. Their chemical alkylating activity compared with the clinical drug CCNU and an experimental compound Mitonafide indicated that they possess lower alkylating activity than CCNU and comparable activity with the latter. Their anti-tumor efficacies were assessed in vivo in two murine ascites tumors namely Sarcoma-180 (S-180) and Ehrlich ascites carcinoma (EAC) by measuring the increase in median survival times (MST) of drug treated (T) over untreated control (C) mice. CCNU and Mitonafide were used as positive controls for comparison. The representative compound 3a has displayed marginal anti-tumoral activity in these tumors. Three compounds were further screened in vitro in 4 different human tumor cell lines but no significant activity was observed in those lines. These compounds moderately inhibit the synthesis of DNA and RNA in S-180 tumor cells.</abstract><cop>Poland</cop><pmid>17665847</pmid></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0001-6837 |
| ispartof | Acta Poloniae pharmaceutica, 2007-01, Vol.64 (1), p.27 |
| issn | 0001-6837 |
| language | eng |
| recordid | cdi_pubmed_primary_17665847 |
| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Animals Antineoplastic Agents, Alkylating - chemical synthesis Antineoplastic Agents, Alkylating - chemistry Antineoplastic Agents, Alkylating - pharmacology Carcinoma, Ehrlich Tumor - drug therapy Cell Line, Tumor DNA - biosynthesis DNA - drug effects Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Imides - pharmacology Isoquinolines - pharmacology Lomustine - pharmacology Mice Naphthalimides - chemical synthesis Naphthalimides - chemistry Naphthalimides - pharmacology Nitrosourea Compounds - administration & dosage Nitrosourea Compounds - chemical synthesis Nitrosourea Compounds - chemistry Nitrosourea Compounds - pharmacology RNA - biosynthesis RNA - drug effects Sarcoma 180 - drug therapy Structure-Activity Relationship |
| title | Synthesis and evaluation of ethylnitrosoureas of substituted naphthalimides as anticancer compounds |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-06T17%3A58%3A33IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-pubmed&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Synthesis%20and%20evaluation%20of%20ethylnitrosoureas%20of%20substituted%20naphthalimides%20as%20anticancer%20compounds&rft.jtitle=Acta%20Poloniae%20pharmaceutica&rft.au=Pain,%20Anindita&rft.date=2007-01&rft.volume=64&rft.issue=1&rft.spage=27&rft.pages=27-&rft.issn=0001-6837&rft_id=info:doi/&rft_dat=%3Cpubmed%3E17665847%3C/pubmed%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/17665847&rfr_iscdi=true |