Synthesis and Antitumor Activities of 1,3,4-Thiadiazole Derivatives Possessing Benzisoselenazolone Scaffold
A series of novel 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold were designed and synthesized, and their antitumor activities against human cervix adenocarcinoma（HeLa）, human liver cancer cell（SMMC-7721）, human breast cancer cell（MCF-7） and human lung cancer cell（A549） lines...
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| Veröffentlicht in: | Chemical research in Chinese universities 2014-10, Vol.30 (5), p.764-769 |
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| creator | Zhao, Jie Xuan, Lina Zhao, Haichuan Cheng, Ji Fu, Xiaoyun Li, Sha Jing, Fen Liu, Yuming Chen, Baoquan |
| description | A series of novel 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold were designed and synthesized, and their antitumor activities against human cervix adenocarcinoma（HeLa）, human liver cancer cell（SMMC-7721）, human breast cancer cell（MCF-7） and human lung cancer cell（A549） lines were evaluated by CCK-8 assay, The bioassay results demonstrate that most of the tested compounds showed potent antiproliferative effects against various cell lines. Furthermore, compounds 7c, 7e, 7h, 7i and 7k showed significant antiproliferative activities against SMMC-7721 cells, with IC5o values of 2.38, 2.67, 1.35, 2.75 and 2.48 μmol/L, respectively. Com- pounds 7a, 7e, 7j and 71 exhibited highly effective antitumor activities against MCF-7 cells, with IC50 values of 2.89, 2.95, 1.12 and 2.75 μmol/L, respectively. Compound 7j was found to be the most potent compound against A549 cells, with an IC50 value of 1.25 μmol/L. The pharmacological results suggest that the substituents of benzylthio-moiety at position 2 on 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines. |
| doi_str_mv | 10.1007/s40242-014-4080-4 |
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Furthermore, compounds 7c, 7e, 7h, 7i and 7k showed significant antiproliferative activities against SMMC-7721 cells, with IC5o values of 2.38, 2.67, 1.35, 2.75 and 2.48 μmol/L, respectively. Com- pounds 7a, 7e, 7j and 71 exhibited highly effective antitumor activities against MCF-7 cells, with IC50 values of 2.89, 2.95, 1.12 and 2.75 μmol/L, respectively. Compound 7j was found to be the most potent compound against A549 cells, with an IC50 value of 1.25 μmol/L. The pharmacological results suggest that the substituents of benzylthio-moiety at position 2 on 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines.</description><identifier>ISSN: 1005-9040</identifier><identifier>EISSN: 2210-3171</identifier><identifier>DOI: 10.1007/s40242-014-4080-4</identifier><language>eng</language><publisher>Changchun: Jilin University and The Editorial Department of Chemical Research in Chinese Universities</publisher><subject>Analytical Chemistry ; Chemistry ; Chemistry and Materials Science ; Chemistry/Food Science ; HeLa细胞 ; Inorganic Chemistry ; MCF-7细胞 ; Organic Chemistry ; Physical Chemistry ; SMMC-7721细胞 ; 人乳腺癌细胞 ; 合成 ; 噻二唑衍生物 ; 抗肿瘤活性 ; 脚手架</subject><ispartof>Chemical research in Chinese universities, 2014-10, Vol.30 (5), p.764-769</ispartof><rights>Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH 2014</rights><rights>Copyright © Wanfang Data Co. 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Res. Chin. Univ</addtitle><addtitle>Chemical Research in Chinese University</addtitle><description>A series of novel 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold were designed and synthesized, and their antitumor activities against human cervix adenocarcinoma（HeLa）, human liver cancer cell（SMMC-7721）, human breast cancer cell（MCF-7） and human lung cancer cell（A549） lines were evaluated by CCK-8 assay, The bioassay results demonstrate that most of the tested compounds showed potent antiproliferative effects against various cell lines. Furthermore, compounds 7c, 7e, 7h, 7i and 7k showed significant antiproliferative activities against SMMC-7721 cells, with IC5o values of 2.38, 2.67, 1.35, 2.75 and 2.48 μmol/L, respectively. Com- pounds 7a, 7e, 7j and 71 exhibited highly effective antitumor activities against MCF-7 cells, with IC50 values of 2.89, 2.95, 1.12 and 2.75 μmol/L, respectively. Compound 7j was found to be the most potent compound against A549 cells, with an IC50 value of 1.25 μmol/L. The pharmacological results suggest that the substituents of benzylthio-moiety at position 2 on 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines.</description><subject>Analytical Chemistry</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Chemistry/Food Science</subject><subject>HeLa细胞</subject><subject>Inorganic Chemistry</subject><subject>MCF-7细胞</subject><subject>Organic Chemistry</subject><subject>Physical Chemistry</subject><subject>SMMC-7721细胞</subject><subject>人乳腺癌细胞</subject><subject>合成</subject><subject>噻二唑衍生物</subject><subject>抗肿瘤活性</subject><subject>脚手架</subject><issn>1005-9040</issn><issn>2210-3171</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><recordid>eNp9kEtPGzEUha0KpIbHD-huxA4phutH7PEyTXlJkUAC1paZuZ44Tex2PNCEX4-joHbX1d183zm6h5BvDC4YgL7MErjkFJikEmqg8gsZcc6ACqbZARkVaEINSPhKjnJeAgijlByRn4_bOCwwh1y52FbTOIThdZ36atoM4S0MAXOVfMXGYizp0yK4Nrj3tMLqB_bhzRWmAA8pZ8w5xK76jvE95JRxhXEHpojVY-O8T6v2hBx6t8p4-nmPyfP11dPsls7vb-5m0zlthDQDRfSodY2guKhrNK0QwI3T8kWwWhnla1bymtYw4VkD2ijUL8JwoUE3tTTimJzvc_-46F3s7DK99rE02q7dbBab7ZKXnWACjBeW7dmmL0_06O2vPqxdv7UM7G5Zu1_WFsPulrWyOHzv5MLGDvt_Bf-Tzj6LFil2v4v3t0kproScKCM-ADbYh7M</recordid><startdate>20141001</startdate><enddate>20141001</enddate><creator>Zhao, Jie</creator><creator>Xuan, Lina</creator><creator>Zhao, Haichuan</creator><creator>Cheng, Ji</creator><creator>Fu, Xiaoyun</creator><creator>Li, Sha</creator><creator>Jing, Fen</creator><creator>Liu, Yuming</creator><creator>Chen, Baoquan</creator><general>Jilin University and The Editorial Department of Chemical Research in Chinese Universities</general><general>School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, P.R.China</general><scope>2RA</scope><scope>92L</scope><scope>CQIGP</scope><scope>~WA</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>2B.</scope><scope>4A8</scope><scope>92I</scope><scope>93N</scope><scope>PSX</scope><scope>TCJ</scope></search><sort><creationdate>20141001</creationdate><title>Synthesis and Antitumor Activities of 1,3,4-Thiadiazole Derivatives Possessing Benzisoselenazolone Scaffold</title><author>Zhao, Jie ; Xuan, Lina ; Zhao, Haichuan ; Cheng, Ji ; Fu, Xiaoyun ; Li, Sha ; Jing, Fen ; Liu, Yuming ; Chen, Baoquan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c349t-eefe778e062388e9d33029a74b318696f81affcd913f1c0796e7b3923707c8493</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Analytical Chemistry</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Chemistry/Food Science</topic><topic>HeLa细胞</topic><topic>Inorganic Chemistry</topic><topic>MCF-7细胞</topic><topic>Organic Chemistry</topic><topic>Physical Chemistry</topic><topic>SMMC-7721细胞</topic><topic>人乳腺癌细胞</topic><topic>合成</topic><topic>噻二唑衍生物</topic><topic>抗肿瘤活性</topic><topic>脚手架</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhao, Jie</creatorcontrib><creatorcontrib>Xuan, Lina</creatorcontrib><creatorcontrib>Zhao, Haichuan</creatorcontrib><creatorcontrib>Cheng, Ji</creatorcontrib><creatorcontrib>Fu, Xiaoyun</creatorcontrib><creatorcontrib>Li, Sha</creatorcontrib><creatorcontrib>Jing, Fen</creatorcontrib><creatorcontrib>Liu, Yuming</creatorcontrib><creatorcontrib>Chen, Baoquan</creatorcontrib><collection>中文科技期刊数据库</collection><collection>中文科技期刊数据库-CALIS站点</collection><collection>中文科技期刊数据库-7.0平台</collection><collection>中文科技期刊数据库- 镜像站点</collection><collection>CrossRef</collection><collection>Wanfang Data Journals - Hong Kong</collection><collection>WANFANG Data Centre</collection><collection>Wanfang Data Journals</collection><collection>万方数据期刊 - 香港版</collection><collection>China Online Journals (COJ)</collection><collection>China Online Journals (COJ)</collection><jtitle>Chemical research in Chinese universities</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhao, Jie</au><au>Xuan, Lina</au><au>Zhao, Haichuan</au><au>Cheng, Ji</au><au>Fu, Xiaoyun</au><au>Li, Sha</au><au>Jing, Fen</au><au>Liu, Yuming</au><au>Chen, Baoquan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and Antitumor Activities of 1,3,4-Thiadiazole Derivatives Possessing Benzisoselenazolone Scaffold</atitle><jtitle>Chemical research in Chinese universities</jtitle><stitle>Chem. Res. Chin. Univ</stitle><addtitle>Chemical Research in Chinese University</addtitle><date>2014-10-01</date><risdate>2014</risdate><volume>30</volume><issue>5</issue><spage>764</spage><epage>769</epage><pages>764-769</pages><issn>1005-9040</issn><eissn>2210-3171</eissn><abstract>A series of novel 1,3,4-thiadiazole derivatives possessing benzisoselenazolone scaffold were designed and synthesized, and their antitumor activities against human cervix adenocarcinoma（HeLa）, human liver cancer cell（SMMC-7721）, human breast cancer cell（MCF-7） and human lung cancer cell（A549） lines were evaluated by CCK-8 assay, The bioassay results demonstrate that most of the tested compounds showed potent antiproliferative effects against various cell lines. Furthermore, compounds 7c, 7e, 7h, 7i and 7k showed significant antiproliferative activities against SMMC-7721 cells, with IC5o values of 2.38, 2.67, 1.35, 2.75 and 2.48 μmol/L, respectively. Com- pounds 7a, 7e, 7j and 71 exhibited highly effective antitumor activities against MCF-7 cells, with IC50 values of 2.89, 2.95, 1.12 and 2.75 μmol/L, respectively. Compound 7j was found to be the most potent compound against A549 cells, with an IC50 value of 1.25 μmol/L. The pharmacological results suggest that the substituents of benzylthio-moiety at position 2 on 1,3,4-thiadiazole are vital for modulating antitumor activities against various cancer cell lines.</abstract><cop>Changchun</cop><pub>Jilin University and The Editorial Department of Chemical Research in Chinese Universities</pub><doi>10.1007/s40242-014-4080-4</doi><tpages>6</tpages></addata></record> |
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| subjects | Analytical Chemistry Chemistry Chemistry and Materials Science Chemistry/Food Science HeLa细胞 Inorganic Chemistry MCF-7细胞 Organic Chemistry Physical Chemistry SMMC-7721细胞 人乳腺癌细胞 合成 噻二唑衍生物 抗肿瘤活性 脚手架 |
| title | Synthesis and Antitumor Activities of 1,3,4-Thiadiazole Derivatives Possessing Benzisoselenazolone Scaffold |
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