Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 권영주 | * |
dc.date.accessioned | 2016-08-27T04:08:04Z | - |
dc.date.available | 2016-08-27T04:08:04Z | - |
dc.date.issued | 2015 | * |
dc.identifier.issn | 0223-5234 | * |
dc.identifier.issn | 1768-3254 | * |
dc.identifier.other | OAK-15553 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/217559 | - |
dc.description.abstract | A series of 2-arylquinazolinones with structural homology to known 3-arylisoquinolines were designed and synthesized in order to develop safe, effective, and selective cytotoxic agents targeting top-oisomerases (topos). 2-Arylquinzolinones with various substitutions on the aromatic rings were obtained by thermal cyclodehydration/dehydrogenation on reacting anthranilamides and benzaldehydes. The compounds had superior topo I-inhibitory activities but were generally inactive against topo II alpha. Among the 6-methyl-, 6-amino-, and 7-methylquinazolinones, 6-amino-substituted derivatives displayed potent cytotoxicity at submicromolar to nanomolar concentrations against human colorectal adenocarcinoma cells (HCT-15), human ductal breast epithelial tumor cells (T47D), and cervical cancer cells (HeLa). There was a good correlation between topo I inhibition and the cytotoxic effects of 6-aminoquinazolinones. Docking models demonstrated that topo I inhibition by these compounds is owing to intercalation and H-bond interactions with the DNA bases and amino acid residues at the enzymatic site. (C) 2015 Elsevier Masson SAS. All rights reserved. | * |
dc.language | English | * |
dc.publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | * |
dc.subject | 2-Arylquinazolinone | * |
dc.subject | 3-Arylisoquinoline | * |
dc.subject | Topoisomerase | * |
dc.subject | Cytotoxicity | * |
dc.subject | Molecular docking | * |
dc.title | Substituted 2-arylquinazolinones: Design, synthesis, and evaluation of cytotoxicity and inhibition of topoisomerases | * |
dc.type | Article | * |
dc.relation.volume | 103 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 69 | * |
dc.relation.lastpage | 79 | * |
dc.relation.journaltitle | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.ejmech.2015.08.040 | * |
dc.identifier.wosid | WOS:000363344700006 | * |
dc.identifier.scopusid | 2-s2.0-84940478437 | * |
dc.author.google | Khadka, Daulat Bikram | * |
dc.author.google | Giap Huu Tran | * |
dc.author.google | Shin, Somin | * |
dc.author.google | Hang Thi Minh Nguyen | * |
dc.author.google | Hue Thi Cao | * |
dc.author.google | Zhao, Chao | * |
dc.author.google | Jin, Yifeng | * |
dc.author.google | Hue Thi My Van | * |
dc.author.google | Minh Van Chau | * |
dc.author.google | Kwon, Youngjoo | * |
dc.author.google | Thanh Nguyen Le | * |
dc.author.google | Cho, Won-Jea | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.date.modifydate | 20240422124907 | * |