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Novel hybrids of drug with bioactive heterocycles for enhancing biological activity
A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised 6a – j . The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies agains...
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| Published in: | Archives of pharmacal research 2016, 39(10), , pp.1382-1390 |
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| Main Authors: | , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c378t-766e8db6e6cb059cb020a1327dec57a6ea75cb2b75432291be1a69400df107a03 |
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| cites | cdi_FETCH-LOGICAL-c378t-766e8db6e6cb059cb020a1327dec57a6ea75cb2b75432291be1a69400df107a03 |
| container_end_page | 1390 |
| container_issue | 10 |
| container_start_page | 1382 |
| container_title | Archives of pharmacal research |
| container_volume | 39 |
| creator | Valentina, Parthiban Ilango, Kaliappan Kathiravan, Muthu K. |
| description | A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised
6a
–
j
. The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA‐1, OAW‐42, T47-D and MCF‐7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains. |
| doi_str_mv | 10.1007/s12272-016-0797-6 |
| format | article |
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6a
–
j
. The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA‐1, OAW‐42, T47-D and MCF‐7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains.</description><identifier>ISSN: 0253-6269</identifier><identifier>EISSN: 1976-3786</identifier><identifier>DOI: 10.1007/s12272-016-0797-6</identifier><identifier>PMID: 27469336</identifier><language>eng</language><publisher>Seoul: Pharmaceutical Society of Korea</publisher><subject>Antifungal Agents - chemistry ; Antifungal Agents - pharmacology ; Aspergillus niger - drug effects ; Aspergillus niger - physiology ; Biological Products - chemistry ; Biological Products - pharmacology ; Candida albicans - drug effects ; Candida albicans - physiology ; Heterocyclic Compounds - chemistry ; Heterocyclic Compounds - pharmacology ; Humans ; MCF-7 Cells ; Medicine ; Pharmacology/Toxicology ; Pharmacy ; Research Article ; Structure-Activity Relationship ; Thiadiazoles - chemistry ; Thiadiazoles - pharmacology ; Triazoles - chemistry ; Triazoles - pharmacology ; 약학</subject><ispartof>Archives of Pharmacal Research, 2016, 39(10), , pp.1382-1390</ispartof><rights>The Pharmaceutical Society of Korea 2016</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c378t-766e8db6e6cb059cb020a1327dec57a6ea75cb2b75432291be1a69400df107a03</citedby><cites>FETCH-LOGICAL-c378t-766e8db6e6cb059cb020a1327dec57a6ea75cb2b75432291be1a69400df107a03</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27469336$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.kci.go.kr/kciportal/ci/sereArticleSearch/ciSereArtiView.kci?sereArticleSearchBean.artiId=ART002155963$$DAccess content in National Research Foundation of Korea (NRF)$$Hfree_for_read</backlink></links><search><creatorcontrib>Valentina, Parthiban</creatorcontrib><creatorcontrib>Ilango, Kaliappan</creatorcontrib><creatorcontrib>Kathiravan, Muthu K.</creatorcontrib><title>Novel hybrids of drug with bioactive heterocycles for enhancing biological activity</title><title>Archives of pharmacal research</title><addtitle>Arch. Pharm. Res</addtitle><addtitle>Arch Pharm Res</addtitle><description>A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised
6a
–
j
. The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA‐1, OAW‐42, T47-D and MCF‐7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains.</description><subject>Antifungal Agents - chemistry</subject><subject>Antifungal Agents - pharmacology</subject><subject>Aspergillus niger - drug effects</subject><subject>Aspergillus niger - physiology</subject><subject>Biological Products - chemistry</subject><subject>Biological Products - pharmacology</subject><subject>Candida albicans - drug effects</subject><subject>Candida albicans - physiology</subject><subject>Heterocyclic Compounds - chemistry</subject><subject>Heterocyclic Compounds - pharmacology</subject><subject>Humans</subject><subject>MCF-7 Cells</subject><subject>Medicine</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Research Article</subject><subject>Structure-Activity Relationship</subject><subject>Thiadiazoles - chemistry</subject><subject>Thiadiazoles - pharmacology</subject><subject>Triazoles - chemistry</subject><subject>Triazoles - pharmacology</subject><subject>약학</subject><issn>0253-6269</issn><issn>1976-3786</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><recordid>eNp9kE1P3DAQhq2qqCy0P6CXysdyCPhjPd4cEWoBaQUS0LPlOJOsl2y8tRPQ_nu8ZOmxl5nDPO-r0UPId87OOWP6InEhtCgYh4LpUhfwicx4qaGQegGfyYwJJQsQUB6Tk5TWjElQSn0hx0LPoZQSZuTxLrxgR1e7Kvo60dDQOo4tffXDilY-WDf4F6QrHDAGt3MdJtqESLFf2d75vt1DXWi9sx19h_2w-0qOGtsl_HbYp-TP719PVzfF8v769upyWbj831BoAFzUFSC4iqkyD8Esl0LX6JS2gFYrV4lKq7kUouQVcgvlnLG64UxbJk_J2dTbx8Y8O2-C9e-7DeY5msuHp1vDBWg-V5n9ObHbGP6OmAaz8clh19kew5gMX2RQalnqjPIJdTGkFLEx2-g3Nu4MZ2bv3UzeTfZu9t4N5MyPQ_1YbbD-l_gQnQExASmf-hajWYcx9lnPf1rfAAMujZU</recordid><startdate>20161001</startdate><enddate>20161001</enddate><creator>Valentina, Parthiban</creator><creator>Ilango, Kaliappan</creator><creator>Kathiravan, Muthu K.</creator><general>Pharmaceutical Society of Korea</general><general>대한약학회</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><scope>ACYCR</scope></search><sort><creationdate>20161001</creationdate><title>Novel hybrids of drug with bioactive heterocycles for enhancing biological activity</title><author>Valentina, Parthiban ; Ilango, Kaliappan ; Kathiravan, Muthu K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c378t-766e8db6e6cb059cb020a1327dec57a6ea75cb2b75432291be1a69400df107a03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Antifungal Agents - chemistry</topic><topic>Antifungal Agents - pharmacology</topic><topic>Aspergillus niger - drug effects</topic><topic>Aspergillus niger - physiology</topic><topic>Biological Products - chemistry</topic><topic>Biological Products - pharmacology</topic><topic>Candida albicans - drug effects</topic><topic>Candida albicans - physiology</topic><topic>Heterocyclic Compounds - chemistry</topic><topic>Heterocyclic Compounds - pharmacology</topic><topic>Humans</topic><topic>MCF-7 Cells</topic><topic>Medicine</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Research Article</topic><topic>Structure-Activity Relationship</topic><topic>Thiadiazoles - chemistry</topic><topic>Thiadiazoles - pharmacology</topic><topic>Triazoles - chemistry</topic><topic>Triazoles - pharmacology</topic><topic>약학</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Valentina, Parthiban</creatorcontrib><creatorcontrib>Ilango, Kaliappan</creatorcontrib><creatorcontrib>Kathiravan, Muthu K.</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><collection>Korean Citation Index</collection><jtitle>Archives of pharmacal research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Valentina, Parthiban</au><au>Ilango, Kaliappan</au><au>Kathiravan, Muthu K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel hybrids of drug with bioactive heterocycles for enhancing biological activity</atitle><jtitle>Archives of pharmacal research</jtitle><stitle>Arch. Pharm. Res</stitle><addtitle>Arch Pharm Res</addtitle><date>2016-10-01</date><risdate>2016</risdate><volume>39</volume><issue>10</issue><spage>1382</spage><epage>1390</epage><pages>1382-1390</pages><issn>0253-6269</issn><eissn>1976-3786</eissn><abstract>A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised
6a
–
j
. The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA‐1, OAW‐42, T47-D and MCF‐7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains.</abstract><cop>Seoul</cop><pub>Pharmaceutical Society of Korea</pub><pmid>27469336</pmid><doi>10.1007/s12272-016-0797-6</doi><tpages>9</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0253-6269 |
| ispartof | Archives of Pharmacal Research, 2016, 39(10), , pp.1382-1390 |
| issn | 0253-6269 1976-3786 |
| language | eng |
| recordid | cdi_nrf_kci_oai_kci_go_kr_ARTI_1267145 |
| source | Springer Nature |
| subjects | Antifungal Agents - chemistry Antifungal Agents - pharmacology Aspergillus niger - drug effects Aspergillus niger - physiology Biological Products - chemistry Biological Products - pharmacology Candida albicans - drug effects Candida albicans - physiology Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Humans MCF-7 Cells Medicine Pharmacology/Toxicology Pharmacy Research Article Structure-Activity Relationship Thiadiazoles - chemistry Thiadiazoles - pharmacology Triazoles - chemistry Triazoles - pharmacology 약학 |
| title | Novel hybrids of drug with bioactive heterocycles for enhancing biological activity |
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