Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives
Background Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotre...
Gespeichert in:
| Veröffentlicht in: | Cancer chemotherapy and pharmacology 2017-11, Vol.80 (5), p.1027-1042 |
|---|---|
| Hauptverfasser: | , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1042 |
|---|---|
| container_issue | 5 |
| container_start_page | 1027 |
| container_title | Cancer chemotherapy and pharmacology |
| container_volume | 80 |
| creator | Khanam, Rashmin Ahmad, Kamal Hejazi, Iram I. Siddique, Ibrar A. Kumar, Vikash Bhat, Abdul Roouf Azam, Amir Athar, Fareeda |
| description | Background
Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotrexate, Vincristine remains limited due to high toxicity, side effects and developing drug resistance. Apoptosis is a crucial cellular process and improper regulation of apoptotic signaling pathways may lead to cancer formation. Subsequently, the synthesis of effective chemotherapeutic agents that can induce apoptosis in tumor cell has emerged as a significant approach in cancer drug discovery.
Methods
The goal of this work is to develop a potential antitumor agent exerting significant inhibitory effects on cancer cell and low cytotoxicity, for which we focused on the structural features of 1,3,4-oxadiazoles as it a privileged scaffold in modern medicinal chemistry and have the ability to inhibit growth factors, enzymes and kinases potentially involved in the attainment of cellular immortality and carcinogenesis.
Result
In vitro MTT screening assay showed the compound 5-aminophenyl-2-butylthio-1,3,4-oxadiazole (
5e
) showing the highest inhibitory effect against MCF-7 cancer cell with IC
50
value 10.05 ± 1.08 µM while it is much safer and less toxic on normal cell line (HEK-293). The dose-dependent treatment of MCF-7 cells with 5e resulted in inhibition of cell migration in the wound healing assay. The flow-cytometry analysis showed the cells arrested in G0/G1 phase of the cell cycle. Compound
5e
induced apoptosis of MCF-7 cells was characterized using DAPI staining and Annexin V-PE/7-AAD dual binding assay. Reduction of NBT by compound
5e
showed a reduced generation of ROS. Western blotting studies showed high activation of apoptotic protein Caspase3 and decrease in expression of anti-apoptotic protein BCL-2.
Conclusion
Based on the results of in vitro studies, it could be concluded that compound
5e
showed a significant inhibitory growth effect on MCF-7 cells and have the potential to be developed as lead molecule and further structural modifications may result in promising new anticancer agents.
Graphical abstract |
| doi_str_mv | 10.1007/s00280-017-3414-6 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1930486213</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>1930486213</sourcerecordid><originalsourceid>FETCH-LOGICAL-c438t-cc1b1d753c45f32e32a43cd4783deb01a716361de754583e8ac68ed9852ddc043</originalsourceid><addsrcrecordid>eNp1kU1vEzEQhi0EoiHwA7ggS1w41DD-2nWPKKJQqYgLnC2vPWlcbexg76aEG_8chxSEkDhZsp95Z8YPIc85vOYA_ZsKIAww4D2TiivWPSALrqRgYJR8SBYglWK6B3VGntR6CwCKS_mYnAljuJYCFuTHVdrEIU65HOhNyXfThuLejbObYk7UpUDdLu-mXGOlMYXZ_7qPiX5cXbKeepc8FupxHCsdDjThHdXMlcPIBBvm6TBOm5gZP5fniuVvLkT3PY9IA5a4bz32WJ-SR2s3Vnx2fy7Jl8t3n1cf2PWn91ert9fMK2km5j0feOi19EqvpUApnJI-qN7IgANw1_NOdjxgr5U2Eo3zncFwYbQIwYOSS_LqlLsr-euMdbLbWI-Du4R5rpZfSFCmE-2HluTlP-htnktq0zWq4xo63ugl4SfKl1xrwbXdlbhtu1sO9ujHnvzY5sce_diu1by4T56HLYY_Fb-FNECcgNqe0g2Wv1r_N_Un4P2aYA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1961506119</pqid></control><display><type>article</type><title>Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives</title><source>MEDLINE</source><source>SpringerLink Journals - AutoHoldings</source><creator>Khanam, Rashmin ; Ahmad, Kamal ; Hejazi, Iram I. ; Siddique, Ibrar A. ; Kumar, Vikash ; Bhat, Abdul Roouf ; Azam, Amir ; Athar, Fareeda</creator><creatorcontrib>Khanam, Rashmin ; Ahmad, Kamal ; Hejazi, Iram I. ; Siddique, Ibrar A. ; Kumar, Vikash ; Bhat, Abdul Roouf ; Azam, Amir ; Athar, Fareeda</creatorcontrib><description>Background
Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotrexate, Vincristine remains limited due to high toxicity, side effects and developing drug resistance. Apoptosis is a crucial cellular process and improper regulation of apoptotic signaling pathways may lead to cancer formation. Subsequently, the synthesis of effective chemotherapeutic agents that can induce apoptosis in tumor cell has emerged as a significant approach in cancer drug discovery.
Methods
The goal of this work is to develop a potential antitumor agent exerting significant inhibitory effects on cancer cell and low cytotoxicity, for which we focused on the structural features of 1,3,4-oxadiazoles as it a privileged scaffold in modern medicinal chemistry and have the ability to inhibit growth factors, enzymes and kinases potentially involved in the attainment of cellular immortality and carcinogenesis.
Result
In vitro MTT screening assay showed the compound 5-aminophenyl-2-butylthio-1,3,4-oxadiazole (
5e
) showing the highest inhibitory effect against MCF-7 cancer cell with IC
50
value 10.05 ± 1.08 µM while it is much safer and less toxic on normal cell line (HEK-293). The dose-dependent treatment of MCF-7 cells with 5e resulted in inhibition of cell migration in the wound healing assay. The flow-cytometry analysis showed the cells arrested in G0/G1 phase of the cell cycle. Compound
5e
induced apoptosis of MCF-7 cells was characterized using DAPI staining and Annexin V-PE/7-AAD dual binding assay. Reduction of NBT by compound
5e
showed a reduced generation of ROS. Western blotting studies showed high activation of apoptotic protein Caspase3 and decrease in expression of anti-apoptotic protein BCL-2.
Conclusion
Based on the results of in vitro studies, it could be concluded that compound
5e
showed a significant inhibitory growth effect on MCF-7 cells and have the potential to be developed as lead molecule and further structural modifications may result in promising new anticancer agents.
Graphical abstract</description><identifier>ISSN: 0344-5704</identifier><identifier>EISSN: 1432-0843</identifier><identifier>DOI: 10.1007/s00280-017-3414-6</identifier><identifier>PMID: 28815320</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Annexin V ; Anticancer properties ; Antineoplastic Agents - pharmacology ; Antineoplastic drugs ; Antitumor agents ; Apoptosis ; Aromatic compounds ; Assaying ; Bcl-2 protein ; Cancer ; Cancer Research ; Carcinogenesis ; Carcinogens ; Cell cycle ; Cell migration ; Cell Proliferation ; Chemotherapy ; Cytometry ; Cytotoxicity ; Doxorubicin ; Drug discovery ; Drug resistance ; Drugs ; G1 phase ; Global health ; Growth factors ; Humans ; Kinases ; MCF-7 Cells ; Medicine ; Medicine & Public Health ; Methotrexate ; Oncology ; Oxadiazoles ; Oxadiazoles - administration & dosage ; Oxadiazoles - pharmacology ; Oxadiazoles - therapeutic use ; Pharmacology/Toxicology ; Short Communication ; Side effects ; Toxicity ; Vincristine ; Western blotting ; Wound healing</subject><ispartof>Cancer chemotherapy and pharmacology, 2017-11, Vol.80 (5), p.1027-1042</ispartof><rights>Springer-Verlag GmbH Germany 2017</rights><rights>Cancer Chemotherapy and Pharmacology is a copyright of Springer, (2017). All Rights Reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c438t-cc1b1d753c45f32e32a43cd4783deb01a716361de754583e8ac68ed9852ddc043</citedby><cites>FETCH-LOGICAL-c438t-cc1b1d753c45f32e32a43cd4783deb01a716361de754583e8ac68ed9852ddc043</cites><orcidid>0000-0001-8097-7206</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s00280-017-3414-6$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s00280-017-3414-6$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28815320$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Khanam, Rashmin</creatorcontrib><creatorcontrib>Ahmad, Kamal</creatorcontrib><creatorcontrib>Hejazi, Iram I.</creatorcontrib><creatorcontrib>Siddique, Ibrar A.</creatorcontrib><creatorcontrib>Kumar, Vikash</creatorcontrib><creatorcontrib>Bhat, Abdul Roouf</creatorcontrib><creatorcontrib>Azam, Amir</creatorcontrib><creatorcontrib>Athar, Fareeda</creatorcontrib><title>Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives</title><title>Cancer chemotherapy and pharmacology</title><addtitle>Cancer Chemother Pharmacol</addtitle><addtitle>Cancer Chemother Pharmacol</addtitle><description>Background
Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotrexate, Vincristine remains limited due to high toxicity, side effects and developing drug resistance. Apoptosis is a crucial cellular process and improper regulation of apoptotic signaling pathways may lead to cancer formation. Subsequently, the synthesis of effective chemotherapeutic agents that can induce apoptosis in tumor cell has emerged as a significant approach in cancer drug discovery.
Methods
The goal of this work is to develop a potential antitumor agent exerting significant inhibitory effects on cancer cell and low cytotoxicity, for which we focused on the structural features of 1,3,4-oxadiazoles as it a privileged scaffold in modern medicinal chemistry and have the ability to inhibit growth factors, enzymes and kinases potentially involved in the attainment of cellular immortality and carcinogenesis.
Result
In vitro MTT screening assay showed the compound 5-aminophenyl-2-butylthio-1,3,4-oxadiazole (
5e
) showing the highest inhibitory effect against MCF-7 cancer cell with IC
50
value 10.05 ± 1.08 µM while it is much safer and less toxic on normal cell line (HEK-293). The dose-dependent treatment of MCF-7 cells with 5e resulted in inhibition of cell migration in the wound healing assay. The flow-cytometry analysis showed the cells arrested in G0/G1 phase of the cell cycle. Compound
5e
induced apoptosis of MCF-7 cells was characterized using DAPI staining and Annexin V-PE/7-AAD dual binding assay. Reduction of NBT by compound
5e
showed a reduced generation of ROS. Western blotting studies showed high activation of apoptotic protein Caspase3 and decrease in expression of anti-apoptotic protein BCL-2.
Conclusion
Based on the results of in vitro studies, it could be concluded that compound
5e
showed a significant inhibitory growth effect on MCF-7 cells and have the potential to be developed as lead molecule and further structural modifications may result in promising new anticancer agents.
Graphical abstract</description><subject>Annexin V</subject><subject>Anticancer properties</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antineoplastic drugs</subject><subject>Antitumor agents</subject><subject>Apoptosis</subject><subject>Aromatic compounds</subject><subject>Assaying</subject><subject>Bcl-2 protein</subject><subject>Cancer</subject><subject>Cancer Research</subject><subject>Carcinogenesis</subject><subject>Carcinogens</subject><subject>Cell cycle</subject><subject>Cell migration</subject><subject>Cell Proliferation</subject><subject>Chemotherapy</subject><subject>Cytometry</subject><subject>Cytotoxicity</subject><subject>Doxorubicin</subject><subject>Drug discovery</subject><subject>Drug resistance</subject><subject>Drugs</subject><subject>G1 phase</subject><subject>Global health</subject><subject>Growth factors</subject><subject>Humans</subject><subject>Kinases</subject><subject>MCF-7 Cells</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Methotrexate</subject><subject>Oncology</subject><subject>Oxadiazoles</subject><subject>Oxadiazoles - administration & dosage</subject><subject>Oxadiazoles - pharmacology</subject><subject>Oxadiazoles - therapeutic use</subject><subject>Pharmacology/Toxicology</subject><subject>Short Communication</subject><subject>Side effects</subject><subject>Toxicity</subject><subject>Vincristine</subject><subject>Western blotting</subject><subject>Wound healing</subject><issn>0344-5704</issn><issn>1432-0843</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNp1kU1vEzEQhi0EoiHwA7ggS1w41DD-2nWPKKJQqYgLnC2vPWlcbexg76aEG_8chxSEkDhZsp95Z8YPIc85vOYA_ZsKIAww4D2TiivWPSALrqRgYJR8SBYglWK6B3VGntR6CwCKS_mYnAljuJYCFuTHVdrEIU65HOhNyXfThuLejbObYk7UpUDdLu-mXGOlMYXZ_7qPiX5cXbKeepc8FupxHCsdDjThHdXMlcPIBBvm6TBOm5gZP5fniuVvLkT3PY9IA5a4bz32WJ-SR2s3Vnx2fy7Jl8t3n1cf2PWn91ert9fMK2km5j0feOi19EqvpUApnJI-qN7IgANw1_NOdjxgr5U2Eo3zncFwYbQIwYOSS_LqlLsr-euMdbLbWI-Du4R5rpZfSFCmE-2HluTlP-htnktq0zWq4xo63ugl4SfKl1xrwbXdlbhtu1sO9ujHnvzY5sce_diu1by4T56HLYY_Fb-FNECcgNqe0g2Wv1r_N_Un4P2aYA</recordid><startdate>20171101</startdate><enddate>20171101</enddate><creator>Khanam, Rashmin</creator><creator>Ahmad, Kamal</creator><creator>Hejazi, Iram I.</creator><creator>Siddique, Ibrar A.</creator><creator>Kumar, Vikash</creator><creator>Bhat, Abdul Roouf</creator><creator>Azam, Amir</creator><creator>Athar, Fareeda</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature B.V</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>3V.</scope><scope>7TO</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8C1</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>H94</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0001-8097-7206</orcidid></search><sort><creationdate>20171101</creationdate><title>Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives</title><author>Khanam, Rashmin ; Ahmad, Kamal ; Hejazi, Iram I. ; Siddique, Ibrar A. ; Kumar, Vikash ; Bhat, Abdul Roouf ; Azam, Amir ; Athar, Fareeda</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c438t-cc1b1d753c45f32e32a43cd4783deb01a716361de754583e8ac68ed9852ddc043</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Annexin V</topic><topic>Anticancer properties</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Antineoplastic drugs</topic><topic>Antitumor agents</topic><topic>Apoptosis</topic><topic>Aromatic compounds</topic><topic>Assaying</topic><topic>Bcl-2 protein</topic><topic>Cancer</topic><topic>Cancer Research</topic><topic>Carcinogenesis</topic><topic>Carcinogens</topic><topic>Cell cycle</topic><topic>Cell migration</topic><topic>Cell Proliferation</topic><topic>Chemotherapy</topic><topic>Cytometry</topic><topic>Cytotoxicity</topic><topic>Doxorubicin</topic><topic>Drug discovery</topic><topic>Drug resistance</topic><topic>Drugs</topic><topic>G1 phase</topic><topic>Global health</topic><topic>Growth factors</topic><topic>Humans</topic><topic>Kinases</topic><topic>MCF-7 Cells</topic><topic>Medicine</topic><topic>Medicine & Public Health</topic><topic>Methotrexate</topic><topic>Oncology</topic><topic>Oxadiazoles</topic><topic>Oxadiazoles - administration & dosage</topic><topic>Oxadiazoles - pharmacology</topic><topic>Oxadiazoles - therapeutic use</topic><topic>Pharmacology/Toxicology</topic><topic>Short Communication</topic><topic>Side effects</topic><topic>Toxicity</topic><topic>Vincristine</topic><topic>Western blotting</topic><topic>Wound healing</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Khanam, Rashmin</creatorcontrib><creatorcontrib>Ahmad, Kamal</creatorcontrib><creatorcontrib>Hejazi, Iram I.</creatorcontrib><creatorcontrib>Siddique, Ibrar A.</creatorcontrib><creatorcontrib>Kumar, Vikash</creatorcontrib><creatorcontrib>Bhat, Abdul Roouf</creatorcontrib><creatorcontrib>Azam, Amir</creatorcontrib><creatorcontrib>Athar, Fareeda</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Oncogenes and Growth Factors Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Public Health Database</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>MEDLINE - Academic</collection><jtitle>Cancer chemotherapy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Khanam, Rashmin</au><au>Ahmad, Kamal</au><au>Hejazi, Iram I.</au><au>Siddique, Ibrar A.</au><au>Kumar, Vikash</au><au>Bhat, Abdul Roouf</au><au>Azam, Amir</au><au>Athar, Fareeda</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives</atitle><jtitle>Cancer chemotherapy and pharmacology</jtitle><stitle>Cancer Chemother Pharmacol</stitle><addtitle>Cancer Chemother Pharmacol</addtitle><date>2017-11-01</date><risdate>2017</risdate><volume>80</volume><issue>5</issue><spage>1027</spage><epage>1042</epage><pages>1027-1042</pages><issn>0344-5704</issn><eissn>1432-0843</eissn><abstract>Background
Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotrexate, Vincristine remains limited due to high toxicity, side effects and developing drug resistance. Apoptosis is a crucial cellular process and improper regulation of apoptotic signaling pathways may lead to cancer formation. Subsequently, the synthesis of effective chemotherapeutic agents that can induce apoptosis in tumor cell has emerged as a significant approach in cancer drug discovery.
Methods
The goal of this work is to develop a potential antitumor agent exerting significant inhibitory effects on cancer cell and low cytotoxicity, for which we focused on the structural features of 1,3,4-oxadiazoles as it a privileged scaffold in modern medicinal chemistry and have the ability to inhibit growth factors, enzymes and kinases potentially involved in the attainment of cellular immortality and carcinogenesis.
Result
In vitro MTT screening assay showed the compound 5-aminophenyl-2-butylthio-1,3,4-oxadiazole (
5e
) showing the highest inhibitory effect against MCF-7 cancer cell with IC
50
value 10.05 ± 1.08 µM while it is much safer and less toxic on normal cell line (HEK-293). The dose-dependent treatment of MCF-7 cells with 5e resulted in inhibition of cell migration in the wound healing assay. The flow-cytometry analysis showed the cells arrested in G0/G1 phase of the cell cycle. Compound
5e
induced apoptosis of MCF-7 cells was characterized using DAPI staining and Annexin V-PE/7-AAD dual binding assay. Reduction of NBT by compound
5e
showed a reduced generation of ROS. Western blotting studies showed high activation of apoptotic protein Caspase3 and decrease in expression of anti-apoptotic protein BCL-2.
Conclusion
Based on the results of in vitro studies, it could be concluded that compound
5e
showed a significant inhibitory growth effect on MCF-7 cells and have the potential to be developed as lead molecule and further structural modifications may result in promising new anticancer agents.
Graphical abstract</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><pmid>28815320</pmid><doi>10.1007/s00280-017-3414-6</doi><tpages>16</tpages><orcidid>https://orcid.org/0000-0001-8097-7206</orcidid></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0344-5704 |
| ispartof | Cancer chemotherapy and pharmacology, 2017-11, Vol.80 (5), p.1027-1042 |
| issn | 0344-5704 1432-0843 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1930486213 |
| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Annexin V Anticancer properties Antineoplastic Agents - pharmacology Antineoplastic drugs Antitumor agents Apoptosis Aromatic compounds Assaying Bcl-2 protein Cancer Cancer Research Carcinogenesis Carcinogens Cell cycle Cell migration Cell Proliferation Chemotherapy Cytometry Cytotoxicity Doxorubicin Drug discovery Drug resistance Drugs G1 phase Global health Growth factors Humans Kinases MCF-7 Cells Medicine Medicine & Public Health Methotrexate Oncology Oxadiazoles Oxadiazoles - administration & dosage Oxadiazoles - pharmacology Oxadiazoles - therapeutic use Pharmacology/Toxicology Short Communication Side effects Toxicity Vincristine Western blotting Wound healing |
| title | Inhibitory growth evaluation and apoptosis induction in MCF-7 cancer cells by new 5-aryl-2-butylthio-1,3,4-oxadiazole derivatives |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-28T18%3A17%3A07IST&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=Inhibitory%20growth%20evaluation%20and%20apoptosis%20induction%20in%20MCF-7%20cancer%20cells%20by%20new%205-aryl-2-butylthio-1,3,4-oxadiazole%20derivatives&rft.jtitle=Cancer%20chemotherapy%20and%20pharmacology&rft.au=Khanam,%20Rashmin&rft.date=2017-11-01&rft.volume=80&rft.issue=5&rft.spage=1027&rft.epage=1042&rft.pages=1027-1042&rft.issn=0344-5704&rft.eissn=1432-0843&rft_id=info:doi/10.1007/s00280-017-3414-6&rft_dat=%3Cproquest_cross%3E1930486213%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=1961506119&rft_id=info:pmid/28815320&rfr_iscdi=true |