Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies
In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives ( 5a–g ) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer acti...
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| Veröffentlicht in: | Journal of chemical biology 2016-10, Vol.9 (4), p.97-106 |
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| creator | Laxmi, S. Vijaya Anil, P. Rajitha, G. Rao, Asha Jyothi Crooks, Peter A. Rajitha, B. |
| description | In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (
5a–g
) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound
5d
(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound
5d
was active against all the cell lines, it has shown potential activity against leukemia SR (GI
50
: 2.04 μM), non-small cell lung cancer NCI-H522 (GI
50
: 1.36 μM), colon cancer COLO 205 (GI
50
: 1.64 μM), CNS cancer SF-539 (GI
50
: 1.87 μM), melanoma SK-MEL-2 (GI
50
: 1.64 μM), ovarian cancer OVCAR-3 (GI
50
: 1.87 μM), renal cancer RXF 393 (GI
50
: 1.15 μM), prostate cancer PC-3 (GI
50
: 1.90 μM), and breast cancer MDA-MB-468(GI
50
: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound
5a
possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs. |
| doi_str_mv | 10.1007/s12154-016-0154-8 |
| format | Article |
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5a–g
) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound
5d
(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound
5d
was active against all the cell lines, it has shown potential activity against leukemia SR (GI
50
: 2.04 μM), non-small cell lung cancer NCI-H522 (GI
50
: 1.36 μM), colon cancer COLO 205 (GI
50
: 1.64 μM), CNS cancer SF-539 (GI
50
: 1.87 μM), melanoma SK-MEL-2 (GI
50
: 1.64 μM), ovarian cancer OVCAR-3 (GI
50
: 1.87 μM), renal cancer RXF 393 (GI
50
: 1.15 μM), prostate cancer PC-3 (GI
50
: 1.90 μM), and breast cancer MDA-MB-468(GI
50
: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound
5a
possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs.</description><identifier>ISSN: 1864-6158</identifier><identifier>EISSN: 1864-6166</identifier><identifier>DOI: 10.1007/s12154-016-0154-8</identifier><identifier>PMID: 27698947</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Anticancer properties ; Antiinfectives and antibacterials ; Antineoplastic drugs ; Antitumor activity ; Antitumor agents ; Biochemistry ; Biological and Medical Physics ; Biophysics ; Biotechnology ; Breast cancer ; Cancer ; Cell Biology ; Chemistry ; Chemistry and Materials Science ; Cleavage ; Colon ; Colon cancer ; Deoxyribonucleic acid ; Derivatives ; Digestion ; DNA ; Kidney cancer ; Leukemia ; Lung cancer ; Melanoma ; Microorganisms ; Non-small cell lung carcinoma ; Original ; Original Article ; Ovarian cancer ; Pharmacology/Toxicology ; Physical Chemistry ; Prostate cancer ; Synthesis ; Tumor cell lines</subject><ispartof>Journal of chemical biology, 2016-10, Vol.9 (4), p.97-106</ispartof><rights>Springer-Verlag Berlin Heidelberg 2016</rights><rights>Copyright Springer Nature B.V. 2016</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3858-a80a3c25fe3609bee581d3f79b2c0f8c2c70e55a2da567ff8c8222140faf0d5b3</citedby><cites>FETCH-LOGICAL-c3858-a80a3c25fe3609bee581d3f79b2c0f8c2c70e55a2da567ff8c8222140faf0d5b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC5026645/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC5026645/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27922,27923,53789,53791</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27698947$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Laxmi, S. Vijaya</creatorcontrib><creatorcontrib>Anil, P.</creatorcontrib><creatorcontrib>Rajitha, G.</creatorcontrib><creatorcontrib>Rao, Asha Jyothi</creatorcontrib><creatorcontrib>Crooks, Peter A.</creatorcontrib><creatorcontrib>Rajitha, B.</creatorcontrib><title>Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies</title><title>Journal of chemical biology</title><addtitle>J Chem Biol</addtitle><addtitle>J Chem Biol</addtitle><description>In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (
5a–g
) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound
5d
(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound
5d
was active against all the cell lines, it has shown potential activity against leukemia SR (GI
50
: 2.04 μM), non-small cell lung cancer NCI-H522 (GI
50
: 1.36 μM), colon cancer COLO 205 (GI
50
: 1.64 μM), CNS cancer SF-539 (GI
50
: 1.87 μM), melanoma SK-MEL-2 (GI
50
: 1.64 μM), ovarian cancer OVCAR-3 (GI
50
: 1.87 μM), renal cancer RXF 393 (GI
50
: 1.15 μM), prostate cancer PC-3 (GI
50
: 1.90 μM), and breast cancer MDA-MB-468(GI
50
: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound
5a
possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs.</description><subject>Anticancer properties</subject><subject>Antiinfectives and antibacterials</subject><subject>Antineoplastic drugs</subject><subject>Antitumor activity</subject><subject>Antitumor agents</subject><subject>Biochemistry</subject><subject>Biological and Medical Physics</subject><subject>Biophysics</subject><subject>Biotechnology</subject><subject>Breast cancer</subject><subject>Cancer</subject><subject>Cell Biology</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Cleavage</subject><subject>Colon</subject><subject>Colon cancer</subject><subject>Deoxyribonucleic acid</subject><subject>Derivatives</subject><subject>Digestion</subject><subject>DNA</subject><subject>Kidney cancer</subject><subject>Leukemia</subject><subject>Lung cancer</subject><subject>Melanoma</subject><subject>Microorganisms</subject><subject>Non-small cell lung carcinoma</subject><subject>Original</subject><subject>Original Article</subject><subject>Ovarian cancer</subject><subject>Pharmacology/Toxicology</subject><subject>Physical Chemistry</subject><subject>Prostate cancer</subject><subject>Synthesis</subject><subject>Tumor cell lines</subject><issn>1864-6158</issn><issn>1864-6166</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><recordid>eNp1kctuFDEQRS1ERB7wAWxQS2xYpIMfbbeHBVIUQkCKYAGsrWq7POOoxw5290jJ1-NhwvCQWFguu05du-oS8pzRM0Zp_7owzmTXUqbqqoF-RI6YVl2rmFKP97HUh-S4lBtKlZCCPSGHvFcLvej6I2K_3MVphSWUJvlmWgW4T2NwIWLLT7vWhRSxcZjDBqawwfKmgTgFC9FiPv0Zr4PNaQgw1pNr3n06b-yIsIElNmWaXcDylBx4GAs-e9hPyLf3l18vPrTXn68-Xpxft1ZoqVvQFITl0qNQdDEgSs2c8P1i4JZ6bbntKUoJ3IFUva83mnPOOurBUycHcULe7nRv52GNzmKcMozmNoc15DuTIJi_MzGszDJtjKRcqU5WgVcPAjl9n7FMZh2KxXGEiGkuhuk6P9VxLSr68h_0Js051vYMZ5oxpjqhK8V2VB1RKRn9_jOMmq2FZmehqRaarYVmW_Pizy72Fb88qwDfAaWm4hLz76f_r_oDowKn3g</recordid><startdate>20161001</startdate><enddate>20161001</enddate><creator>Laxmi, S. Vijaya</creator><creator>Anil, P.</creator><creator>Rajitha, G.</creator><creator>Rao, Asha Jyothi</creator><creator>Crooks, Peter A.</creator><creator>Rajitha, B.</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature B.V</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QL</scope><scope>7QO</scope><scope>7QP</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20161001</creationdate><title>Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies</title><author>Laxmi, S. Vijaya ; Anil, P. ; Rajitha, G. ; Rao, Asha Jyothi ; Crooks, Peter A. ; Rajitha, B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3858-a80a3c25fe3609bee581d3f79b2c0f8c2c70e55a2da567ff8c8222140faf0d5b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Anticancer properties</topic><topic>Antiinfectives and antibacterials</topic><topic>Antineoplastic drugs</topic><topic>Antitumor activity</topic><topic>Antitumor agents</topic><topic>Biochemistry</topic><topic>Biological and Medical Physics</topic><topic>Biophysics</topic><topic>Biotechnology</topic><topic>Breast cancer</topic><topic>Cancer</topic><topic>Cell Biology</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Cleavage</topic><topic>Colon</topic><topic>Colon cancer</topic><topic>Deoxyribonucleic acid</topic><topic>Derivatives</topic><topic>Digestion</topic><topic>DNA</topic><topic>Kidney cancer</topic><topic>Leukemia</topic><topic>Lung cancer</topic><topic>Melanoma</topic><topic>Microorganisms</topic><topic>Non-small cell lung carcinoma</topic><topic>Original</topic><topic>Original Article</topic><topic>Ovarian cancer</topic><topic>Pharmacology/Toxicology</topic><topic>Physical Chemistry</topic><topic>Prostate cancer</topic><topic>Synthesis</topic><topic>Tumor cell lines</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Laxmi, S. Vijaya</creatorcontrib><creatorcontrib>Anil, P.</creatorcontrib><creatorcontrib>Rajitha, G.</creatorcontrib><creatorcontrib>Rao, Asha Jyothi</creatorcontrib><creatorcontrib>Crooks, Peter A.</creatorcontrib><creatorcontrib>Rajitha, B.</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Journal of chemical biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Laxmi, S. Vijaya</au><au>Anil, P.</au><au>Rajitha, G.</au><au>Rao, Asha Jyothi</au><au>Crooks, Peter A.</au><au>Rajitha, B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies</atitle><jtitle>Journal of chemical biology</jtitle><stitle>J Chem Biol</stitle><addtitle>J Chem Biol</addtitle><date>2016-10-01</date><risdate>2016</risdate><volume>9</volume><issue>4</issue><spage>97</spage><epage>106</epage><pages>97-106</pages><issn>1864-6158</issn><eissn>1864-6166</eissn><abstract>In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (
5a–g
) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound
5d
(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound
5d
was active against all the cell lines, it has shown potential activity against leukemia SR (GI
50
: 2.04 μM), non-small cell lung cancer NCI-H522 (GI
50
: 1.36 μM), colon cancer COLO 205 (GI
50
: 1.64 μM), CNS cancer SF-539 (GI
50
: 1.87 μM), melanoma SK-MEL-2 (GI
50
: 1.64 μM), ovarian cancer OVCAR-3 (GI
50
: 1.87 μM), renal cancer RXF 393 (GI
50
: 1.15 μM), prostate cancer PC-3 (GI
50
: 1.90 μM), and breast cancer MDA-MB-468(GI
50
: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound
5a
possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><pmid>27698947</pmid><doi>10.1007/s12154-016-0154-8</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Anticancer properties Antiinfectives and antibacterials Antineoplastic drugs Antitumor activity Antitumor agents Biochemistry Biological and Medical Physics Biophysics Biotechnology Breast cancer Cancer Cell Biology Chemistry Chemistry and Materials Science Cleavage Colon Colon cancer Deoxyribonucleic acid Derivatives Digestion DNA Kidney cancer Leukemia Lung cancer Melanoma Microorganisms Non-small cell lung carcinoma Original Original Article Ovarian cancer Pharmacology/Toxicology Physical Chemistry Prostate cancer Synthesis Tumor cell lines |
| title | Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies |
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