Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action
[Display omitted] A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic a...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2015-12, Vol.25 (24), p.5772-5776 |
|---|---|
| Hauptverfasser: | , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 5776 |
|---|---|
| container_issue | 24 |
| container_start_page | 5772 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 25 |
| creator | Yu, Xifang Shi, Liqiao Ke, Shaoyong |
| description | [Display omitted]
A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay. |
| doi_str_mv | 10.1016/j.bmcl.2015.10.069 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1735326645</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X15301785</els_id><sourcerecordid>1735326645</sourcerecordid><originalsourceid>FETCH-LOGICAL-c356t-77501fc9e9288b7684fc4010c2900f7fa4161f8901ee740ff5bff6d0d1ec36093</originalsourceid><addsrcrecordid>eNp9kEtLxDAUhYMoOj7-gAvJ0oUdb9o0bcWNiC8QXKjgLqTpjZOxbcakMzD-elNGXbq6cPjOgfsRcsxgyoCJ8_m07nQ7TYHlMZiCqLbIhHHBk4xDvk0mUAlIyoq_7ZH9EOYAjAPnu2QvFTkXKeMT8nGl1-1s3Xj15XqkDXq7UoNdYaAq0IUbsB-saqmKR6teo6fqPWbhgj6v-2GGwYYzWluX4Eq1y1h1fYQb2qGeqd6GjjpDlR7zQ7JjVBvw6OcekNfbm5fr--Tx6e7h-uox0VkuhqQocmBGV1ilZVkXouRGc2Cg0wrAFEZxJpgpK2CIBQdj8toY0UDDUGcCquyAnG52F959LjEMsrNBY9uqHt0ySFZkeZYKwfOIphtUexeCRyMX3nbKryUDOUqWczlKlqPkMYuSY-nkZ39Zd9j8VX6tRuByA2D8cmXRy6AtRnmN9agH2Tj73_43V4iPLA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1735326645</pqid></control><display><type>article</type><title>Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals Complete</source><creator>Yu, Xifang ; Shi, Liqiao ; Ke, Shaoyong</creator><creatorcontrib>Yu, Xifang ; Shi, Liqiao ; Ke, Shaoyong</creatorcontrib><description>[Display omitted]
A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2015.10.069</identifier><identifier>PMID: 26546214</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Acylhydrazone ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - toxicity ; Apoptosis ; Apoptosis - drug effects ; Cell Line, Tumor ; Cytotoxic activity ; Drug Screening Assays, Antitumor ; Fluorouracil - toxicity ; Hep G2 Cells ; Humans ; Hydrazones - chemical synthesis ; Hydrazones - chemistry ; Hydrazones - toxicity ; Synthesis</subject><ispartof>Bioorganic & medicinal chemistry letters, 2015-12, Vol.25 (24), p.5772-5776</ispartof><rights>2015 Elsevier Ltd</rights><rights>Copyright © 2015 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-77501fc9e9288b7684fc4010c2900f7fa4161f8901ee740ff5bff6d0d1ec36093</citedby><cites>FETCH-LOGICAL-c356t-77501fc9e9288b7684fc4010c2900f7fa4161f8901ee740ff5bff6d0d1ec36093</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2015.10.069$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26546214$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yu, Xifang</creatorcontrib><creatorcontrib>Shi, Liqiao</creatorcontrib><creatorcontrib>Ke, Shaoyong</creatorcontrib><title>Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay.</description><subject>Acylhydrazone</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - toxicity</subject><subject>Apoptosis</subject><subject>Apoptosis - drug effects</subject><subject>Cell Line, Tumor</subject><subject>Cytotoxic activity</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Fluorouracil - toxicity</subject><subject>Hep G2 Cells</subject><subject>Humans</subject><subject>Hydrazones - chemical synthesis</subject><subject>Hydrazones - chemistry</subject><subject>Hydrazones - toxicity</subject><subject>Synthesis</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLxDAUhYMoOj7-gAvJ0oUdb9o0bcWNiC8QXKjgLqTpjZOxbcakMzD-elNGXbq6cPjOgfsRcsxgyoCJ8_m07nQ7TYHlMZiCqLbIhHHBk4xDvk0mUAlIyoq_7ZH9EOYAjAPnu2QvFTkXKeMT8nGl1-1s3Xj15XqkDXq7UoNdYaAq0IUbsB-saqmKR6teo6fqPWbhgj6v-2GGwYYzWluX4Eq1y1h1fYQb2qGeqd6GjjpDlR7zQ7JjVBvw6OcekNfbm5fr--Tx6e7h-uox0VkuhqQocmBGV1ilZVkXouRGc2Cg0wrAFEZxJpgpK2CIBQdj8toY0UDDUGcCquyAnG52F959LjEMsrNBY9uqHt0ySFZkeZYKwfOIphtUexeCRyMX3nbKryUDOUqWczlKlqPkMYuSY-nkZ39Zd9j8VX6tRuByA2D8cmXRy6AtRnmN9agH2Tj73_43V4iPLA</recordid><startdate>20151215</startdate><enddate>20151215</enddate><creator>Yu, Xifang</creator><creator>Shi, Liqiao</creator><creator>Ke, Shaoyong</creator><general>Elsevier Ltd</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></search><sort><creationdate>20151215</creationdate><title>Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action</title><author>Yu, Xifang ; Shi, Liqiao ; Ke, Shaoyong</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-77501fc9e9288b7684fc4010c2900f7fa4161f8901ee740ff5bff6d0d1ec36093</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Acylhydrazone</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - toxicity</topic><topic>Apoptosis</topic><topic>Apoptosis - drug effects</topic><topic>Cell Line, Tumor</topic><topic>Cytotoxic activity</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Fluorouracil - toxicity</topic><topic>Hep G2 Cells</topic><topic>Humans</topic><topic>Hydrazones - chemical synthesis</topic><topic>Hydrazones - chemistry</topic><topic>Hydrazones - toxicity</topic><topic>Synthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yu, Xifang</creatorcontrib><creatorcontrib>Shi, Liqiao</creatorcontrib><creatorcontrib>Ke, Shaoyong</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><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yu, Xifang</au><au>Shi, Liqiao</au><au>Ke, Shaoyong</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2015-12-15</date><risdate>2015</risdate><volume>25</volume><issue>24</issue><spage>5772</spage><epage>5776</epage><pages>5772-5776</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>26546214</pmid><doi>10.1016/j.bmcl.2015.10.069</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2015-12, Vol.25 (24), p.5772-5776 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1735326645 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Acylhydrazone Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - toxicity Apoptosis Apoptosis - drug effects Cell Line, Tumor Cytotoxic activity Drug Screening Assays, Antitumor Fluorouracil - toxicity Hep G2 Cells Humans Hydrazones - chemical synthesis Hydrazones - chemistry Hydrazones - toxicity Synthesis |
| title | Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-05T03%3A29%3A15IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Acylhydrazone%20derivatives%20as%20potential%20anticancer%20agents:%20Synthesis,%20bio-evaluation%20and%20mechanism%20of%20action&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Yu,%20Xifang&rft.date=2015-12-15&rft.volume=25&rft.issue=24&rft.spage=5772&rft.epage=5776&rft.pages=5772-5776&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2015.10.069&rft_dat=%3Cproquest_cross%3E1735326645%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1735326645&rft_id=info:pmid/26546214&rft_els_id=S0960894X15301785&rfr_iscdi=true |