dc.contributor.author | Guzelcan, Ece Akhan | |
dc.contributor.author | Ibis, Kamuran | |
dc.contributor.author | Atalay, Rengul Cetin | |
dc.contributor.author | BANOĞLU, ERDEN | |
dc.contributor.author | ÇALIŞKAN, BURCU | |
dc.contributor.author | NALBAT, ESRA | |
dc.date.accessioned | 2021-03-04T12:50:11Z | |
dc.date.available | 2021-03-04T12:50:11Z | |
dc.date.issued | 2018 | |
dc.identifier.citation | ÇALIŞKAN B., NALBAT E., Ibis K., Guzelcan E. A. , Atalay R. C. , BANOĞLU E., "Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.33, sa.1, ss.1352-1361, 2018 | |
dc.identifier.issn | 1475-6366 | |
dc.identifier.other | vv_1032021 | |
dc.identifier.other | av_7958b96c-11d4-4493-80fa-787b7fe841b9 | |
dc.identifier.uri | http://hdl.handle.net/20.500.12627/83172 | |
dc.identifier.uri | https://doi.org/10.1080/14756366.2018.1504041 | |
dc.description.abstract | In our endeavour towards the development of effective anticancer therapeutics, a novel series of isoxazole-piperazine hybrids were synthesized and evaluated for their cytotoxic activities against human liver (Huh7 and Mahlavu) and breast (MCF-7) cancer cell lines. Within series, compounds 51-o showed the most potent cytotoxicity on all cell lines with IC50 values in the range of 0.3-3.7 mu M. To explore the mechanistic aspects fundamental to the observed activity, further biological studies with 5m and 5o in liver cancer cells were carried out. We have demonstrated that 5m and 5o induce oxidative stress in PTEN adequate Huh7 and PTEN deficient Mahlavu human liver cancer cells leading to apoptosis and cell cycle arrest at different phases. Further analysis of the proteins involved in apoptosis and cell cycle revealed that 5m and 5o caused an inhibition of cell survival pathway through Akt hyperphosphorylation and apoptosis and cell cycle arrest through p53 protein activation. | |
dc.language.iso | eng | |
dc.subject | Pharmacology | |
dc.subject | Molecular Biology | |
dc.subject | Drug Discovery | |
dc.subject | Aging | |
dc.subject | General Biochemistry, Genetics and Molecular Biology | |
dc.subject | General Pharmacology, Toxicology and Pharmaceutics | |
dc.subject | Pharmacology, Toxicology and Pharmaceutics (miscellaneous) | |
dc.subject | Biochemistry | |
dc.subject | Structural Biology | |
dc.subject | Chemistry (miscellaneous) | |
dc.subject | Moleküler Biyoloji ve Genetik | |
dc.subject | Pharmacology (medical) | |
dc.subject | Pharmacy | |
dc.subject | Drug Guides | |
dc.subject | Physical Sciences | |
dc.subject | Life Sciences | |
dc.subject | Health Sciences | |
dc.subject | General Chemistry | |
dc.subject | Sitogenetik | |
dc.subject | BİYOKİMYA VE MOLEKÜLER BİYOLOJİ | |
dc.subject | Moleküler Biyoloji ve Genetik | |
dc.subject | Yaşam Bilimleri (LIFE) | |
dc.subject | KİMYA, TIP | |
dc.subject | Kimya | |
dc.subject | Temel Bilimler (SCI) | |
dc.subject | FARMAKOLOJİ VE ECZACILIK | |
dc.subject | Farmakoloji ve Toksikoloji | |
dc.subject | Sağlık Bilimleri | |
dc.subject | Eczacılık | |
dc.subject | Temel Eczacılık Bilimleri | |
dc.subject | Yaşam Bilimleri | |
dc.subject | Biyokimya | |
dc.subject | Temel Bilimler | |
dc.subject | Biochemistry, Genetics and Molecular Biology (miscellaneous) | |
dc.subject | Clinical Biochemistry | |
dc.subject | Cancer Research | |
dc.title | Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents | |
dc.type | Makale | |
dc.relation.journal | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | |
dc.contributor.department | Gazi Üniversitesi , Eczacılık Fakültesi , Eczacılık Meslek Bilimleri | |
dc.identifier.volume | 33 | |
dc.identifier.issue | 1 | |
dc.identifier.startpage | 1352 | |
dc.identifier.endpage | 1361 | |
dc.contributor.firstauthorID | 2497516 | |