{"title":"抗乳腺癌喹唑啉酮衍生物的合成与表征","authors":"Asha Jose , Amrutha Balakrishnan Chittethu , Sathianarayanan Sankaran , Saranya Tulasidharan Suja , Kumar Prem Ekambaram","doi":"10.1016/j.jopr.2013.07.033","DOIUrl":null,"url":null,"abstract":"<div><h3>Aim</h3><p>The present study was aimed to synthesis series of quinazolinone derivatives against mammary carcinoma.</p></div><div><h3>Methods</h3><p>The compounds were synthesized by reaction of nucleophilic attack, Wohler's classical synthesis followed by condensation reaction. The synthesized quinazolinone derivatives were characterized by physico chemical analysis like melting point, TLC, IR, UV and NMR. Compounds have been evaluated for their <em>in-vitro</em> antioxidant methods like DPPH method, H<sub>2</sub>O<sub>2</sub> method, nitrous oxide scavenging method, super oxide scavenging method, ABTS radical scavenging, lipid peroxidation and also <em>in-vitro</em> cytotoxicity study against MCF-7, BT-549, ZR-75 (human breast cancer) cell lines by MTT assay method.</p></div><div><h3>Results</h3><p>From physico chemical data the structure of synthesized compounds was confirmed. Antioxidant activity was found from the IC<sub>50</sub> value. Qc showed lowest IC<sub>50</sub> value in DPPH radical scavenging assay and nitric oxide scavenging assay and was observed to be 27.20 μg/ml and 26.3 μg/ml respectively. In super oxide scavenging activity and lipid peroxidation and H<sub>2</sub>O<sub>2</sub> assays showed a good activity it was observed 26.3 μg/ml, 18.10 μg/ml and 21.4 μg/ml respectively. Qb showed lowest IC<sub>50</sub> value in ABTS radical scavenging assay and was observed to be 26.9 μg/ml. Qe showed lowest IC<sub>50</sub> value in lipid peroxidation method and was observed to be 149 μg/ml. QN-D showed a moderate antioxidant. In cytotoxic activity, Qc showed lowest IC<sub>50</sub> value, i.e. 21.77, 23.03 and 21.14 μg/ml and Qb showed moderate values like 23.25 μg/ml, 27.39 μg/ml and 27.86 μg/ml in MCF-7, BT-549 and ZT-75 respectively.</p></div><div><h3>Conclusion</h3><p>All the synthesized compounds showed moderate to good antioxidant and potent cytotoxic activity.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 9","pages":"Pages 933-938"},"PeriodicalIF":0.0000,"publicationDate":"2013-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.033","citationCount":"4","resultStr":"{\"title\":\"Synthesis and characterization of quinazolinone derivatives against mammary carcinoma\",\"authors\":\"Asha Jose , Amrutha Balakrishnan Chittethu , Sathianarayanan Sankaran , Saranya Tulasidharan Suja , Kumar Prem Ekambaram\",\"doi\":\"10.1016/j.jopr.2013.07.033\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Aim</h3><p>The present study was aimed to synthesis series of quinazolinone derivatives against mammary carcinoma.</p></div><div><h3>Methods</h3><p>The compounds were synthesized by reaction of nucleophilic attack, Wohler's classical synthesis followed by condensation reaction. The synthesized quinazolinone derivatives were characterized by physico chemical analysis like melting point, TLC, IR, UV and NMR. Compounds have been evaluated for their <em>in-vitro</em> antioxidant methods like DPPH method, H<sub>2</sub>O<sub>2</sub> method, nitrous oxide scavenging method, super oxide scavenging method, ABTS radical scavenging, lipid peroxidation and also <em>in-vitro</em> cytotoxicity study against MCF-7, BT-549, ZR-75 (human breast cancer) cell lines by MTT assay method.</p></div><div><h3>Results</h3><p>From physico chemical data the structure of synthesized compounds was confirmed. Antioxidant activity was found from the IC<sub>50</sub> value. Qc showed lowest IC<sub>50</sub> value in DPPH radical scavenging assay and nitric oxide scavenging assay and was observed to be 27.20 μg/ml and 26.3 μg/ml respectively. In super oxide scavenging activity and lipid peroxidation and H<sub>2</sub>O<sub>2</sub> assays showed a good activity it was observed 26.3 μg/ml, 18.10 μg/ml and 21.4 μg/ml respectively. Qb showed lowest IC<sub>50</sub> value in ABTS radical scavenging assay and was observed to be 26.9 μg/ml. Qe showed lowest IC<sub>50</sub> value in lipid peroxidation method and was observed to be 149 μg/ml. QN-D showed a moderate antioxidant. In cytotoxic activity, Qc showed lowest IC<sub>50</sub> value, i.e. 21.77, 23.03 and 21.14 μg/ml and Qb showed moderate values like 23.25 μg/ml, 27.39 μg/ml and 27.86 μg/ml in MCF-7, BT-549 and ZT-75 respectively.</p></div><div><h3>Conclusion</h3><p>All the synthesized compounds showed moderate to good antioxidant and potent cytotoxic activity.</p></div>\",\"PeriodicalId\":16787,\"journal\":{\"name\":\"Journal of Pharmacy Research\",\"volume\":\"6 9\",\"pages\":\"Pages 933-938\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2013-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.033\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmacy Research\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0974694313003587\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmacy Research","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0974694313003587","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and characterization of quinazolinone derivatives against mammary carcinoma
Aim
The present study was aimed to synthesis series of quinazolinone derivatives against mammary carcinoma.
Methods
The compounds were synthesized by reaction of nucleophilic attack, Wohler's classical synthesis followed by condensation reaction. The synthesized quinazolinone derivatives were characterized by physico chemical analysis like melting point, TLC, IR, UV and NMR. Compounds have been evaluated for their in-vitro antioxidant methods like DPPH method, H2O2 method, nitrous oxide scavenging method, super oxide scavenging method, ABTS radical scavenging, lipid peroxidation and also in-vitro cytotoxicity study against MCF-7, BT-549, ZR-75 (human breast cancer) cell lines by MTT assay method.
Results
From physico chemical data the structure of synthesized compounds was confirmed. Antioxidant activity was found from the IC50 value. Qc showed lowest IC50 value in DPPH radical scavenging assay and nitric oxide scavenging assay and was observed to be 27.20 μg/ml and 26.3 μg/ml respectively. In super oxide scavenging activity and lipid peroxidation and H2O2 assays showed a good activity it was observed 26.3 μg/ml, 18.10 μg/ml and 21.4 μg/ml respectively. Qb showed lowest IC50 value in ABTS radical scavenging assay and was observed to be 26.9 μg/ml. Qe showed lowest IC50 value in lipid peroxidation method and was observed to be 149 μg/ml. QN-D showed a moderate antioxidant. In cytotoxic activity, Qc showed lowest IC50 value, i.e. 21.77, 23.03 and 21.14 μg/ml and Qb showed moderate values like 23.25 μg/ml, 27.39 μg/ml and 27.86 μg/ml in MCF-7, BT-549 and ZT-75 respectively.
Conclusion
All the synthesized compounds showed moderate to good antioxidant and potent cytotoxic activity.