Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs
A new series of hybrid 2-Quinolinone derivatives were synthesized and structurally proved using spectral and elemental analyses data. All the prepared compounds were tested for their in vitro cytotoxic activity against MCF-7 cell line. Compounds 6 and 8 showed potent anticancer activity, which were...
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| Veröffentlicht in: | Research on chemical intermediates 2019-07, Vol.45 (7), p.3895-3912 |
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| creator | Moustafa, Amal Mahmoud Youssef Bakare, Safyah B. |
| description | A new series of hybrid 2-Quinolinone derivatives were synthesized and structurally proved using spectral and elemental analyses data. All the prepared compounds were tested for their in vitro cytotoxic activity against MCF-7 cell line. Compounds
6
and
8
showed potent anticancer activity, which were comparable to Doxorubicin as reference compound. While compound 3 was comparable to cisplatin. Cell cycle analysis of compounds
6
and
8
showed cell cycle arrest at S and G
2
/M phases of the cycle and induced apoptosis at pre-G1 phase. DNA synthesis inhibitory activity demonstrated that compound
6
showed equipotent activity to Doxorubicin. The extent of apoptosis was also determined using Annexin V-FITC assay. In addition, compounds
6
and
8
increase the activation of effector caspase 3 by four fold more than untreated control. On the other hand, the localization of compounds 3, 6 and 8 were found in the nucleus. |
| doi_str_mv | 10.1007/s11164-019-03827-y |
| format | Article |
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6
and
8
showed potent anticancer activity, which were comparable to Doxorubicin as reference compound. While compound 3 was comparable to cisplatin. Cell cycle analysis of compounds
6
and
8
showed cell cycle arrest at S and G
2
/M phases of the cycle and induced apoptosis at pre-G1 phase. DNA synthesis inhibitory activity demonstrated that compound
6
showed equipotent activity to Doxorubicin. The extent of apoptosis was also determined using Annexin V-FITC assay. In addition, compounds
6
and
8
increase the activation of effector caspase 3 by four fold more than untreated control. On the other hand, the localization of compounds 3, 6 and 8 were found in the nucleus.</description><identifier>ISSN: 0922-6168</identifier><identifier>EISSN: 1568-5675</identifier><identifier>DOI: 10.1007/s11164-019-03827-y</identifier><language>eng</language><publisher>Dordrecht: Springer Netherlands</publisher><subject>Anticancer properties ; Apoptosis ; Breast cancer ; Catalysis ; Cell cycle ; Chemistry ; Chemistry and Materials Science ; Derivatives ; Doxorubicin ; Inorganic Chemistry ; Physical Chemistry ; Synthesis</subject><ispartof>Research on chemical intermediates, 2019-07, Vol.45 (7), p.3895-3912</ispartof><rights>Springer Nature B.V. 2019</rights><rights>Copyright Springer Nature B.V. 2019</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-ab37b1cf9c2c042fab6ea1e5c5cf13f9f25e30c383bb1a09d83b69df8181fd4f3</citedby><cites>FETCH-LOGICAL-c356t-ab37b1cf9c2c042fab6ea1e5c5cf13f9f25e30c383bb1a09d83b69df8181fd4f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11164-019-03827-y$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11164-019-03827-y$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids></links><search><creatorcontrib>Moustafa, Amal Mahmoud Youssef</creatorcontrib><creatorcontrib>Bakare, Safyah B.</creatorcontrib><title>Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs</title><title>Research on chemical intermediates</title><addtitle>Res Chem Intermed</addtitle><description>A new series of hybrid 2-Quinolinone derivatives were synthesized and structurally proved using spectral and elemental analyses data. All the prepared compounds were tested for their in vitro cytotoxic activity against MCF-7 cell line. Compounds
6
and
8
showed potent anticancer activity, which were comparable to Doxorubicin as reference compound. While compound 3 was comparable to cisplatin. Cell cycle analysis of compounds
6
and
8
showed cell cycle arrest at S and G
2
/M phases of the cycle and induced apoptosis at pre-G1 phase. DNA synthesis inhibitory activity demonstrated that compound
6
showed equipotent activity to Doxorubicin. The extent of apoptosis was also determined using Annexin V-FITC assay. In addition, compounds
6
and
8
increase the activation of effector caspase 3 by four fold more than untreated control. On the other hand, the localization of compounds 3, 6 and 8 were found in the nucleus.</description><subject>Anticancer properties</subject><subject>Apoptosis</subject><subject>Breast cancer</subject><subject>Catalysis</subject><subject>Cell cycle</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Derivatives</subject><subject>Doxorubicin</subject><subject>Inorganic Chemistry</subject><subject>Physical Chemistry</subject><subject>Synthesis</subject><issn>0922-6168</issn><issn>1568-5675</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><recordid>eNp9kM9LwzAUx4MoOKf_gKeA52he0qTpcW7qhIHI1GtI02R2bO1MumH_e6MVvAnv8d7h-wM-CF0CvQZK85sIADIjFApCuWI56Y_QCIRURMhcHKMRLRgjEqQ6RWcxrikFoRQdobdl33TvLtYRtx4v263D874MdYVzMu-r0H72-HlfN-0mbePwzIX6YLr64CKepGm6Gt8GZ2KHp6axLuBZ2K_iOTrxZhPdxe8do9f7u5fpnCyeHh6nkwWxXMiOmJLnJVhfWGZpxrwppTPghBXWA_eFZ8JxarniZQmGFlV6ZFF5BQp8lXk-RldD7i60H3sXO71u96FJlZoxngmRUkVSsUFlQxtjcF7vQr01oddA9Tc_PfDTiZ_-4af7ZOKDKSZxs3LhL_of1xeod3Q_</recordid><startdate>20190715</startdate><enddate>20190715</enddate><creator>Moustafa, Amal Mahmoud Youssef</creator><creator>Bakare, Safyah B.</creator><general>Springer Netherlands</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20190715</creationdate><title>Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs</title><author>Moustafa, Amal Mahmoud Youssef ; Bakare, Safyah B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-ab37b1cf9c2c042fab6ea1e5c5cf13f9f25e30c383bb1a09d83b69df8181fd4f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Anticancer properties</topic><topic>Apoptosis</topic><topic>Breast cancer</topic><topic>Catalysis</topic><topic>Cell cycle</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Derivatives</topic><topic>Doxorubicin</topic><topic>Inorganic Chemistry</topic><topic>Physical Chemistry</topic><topic>Synthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Moustafa, Amal Mahmoud Youssef</creatorcontrib><creatorcontrib>Bakare, Safyah B.</creatorcontrib><collection>CrossRef</collection><jtitle>Research on chemical intermediates</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Moustafa, Amal Mahmoud Youssef</au><au>Bakare, Safyah B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs</atitle><jtitle>Research on chemical intermediates</jtitle><stitle>Res Chem Intermed</stitle><date>2019-07-15</date><risdate>2019</risdate><volume>45</volume><issue>7</issue><spage>3895</spage><epage>3912</epage><pages>3895-3912</pages><issn>0922-6168</issn><eissn>1568-5675</eissn><abstract>A new series of hybrid 2-Quinolinone derivatives were synthesized and structurally proved using spectral and elemental analyses data. All the prepared compounds were tested for their in vitro cytotoxic activity against MCF-7 cell line. Compounds
6
and
8
showed potent anticancer activity, which were comparable to Doxorubicin as reference compound. While compound 3 was comparable to cisplatin. Cell cycle analysis of compounds
6
and
8
showed cell cycle arrest at S and G
2
/M phases of the cycle and induced apoptosis at pre-G1 phase. DNA synthesis inhibitory activity demonstrated that compound
6
showed equipotent activity to Doxorubicin. The extent of apoptosis was also determined using Annexin V-FITC assay. In addition, compounds
6
and
8
increase the activation of effector caspase 3 by four fold more than untreated control. On the other hand, the localization of compounds 3, 6 and 8 were found in the nucleus.</abstract><cop>Dordrecht</cop><pub>Springer Netherlands</pub><doi>10.1007/s11164-019-03827-y</doi><tpages>18</tpages></addata></record> |
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| ispartof | Research on chemical intermediates, 2019-07, Vol.45 (7), p.3895-3912 |
| issn | 0922-6168 1568-5675 |
| language | eng |
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| subjects | Anticancer properties Apoptosis Breast cancer Catalysis Cell cycle Chemistry Chemistry and Materials Science Derivatives Doxorubicin Inorganic Chemistry Physical Chemistry Synthesis |
| title | Synthesis of Some Hybrid 7-Hydroxy Quinolinone Derivatives As Anti Breast Cancer Drugs |
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