Design, synthesis and bioevaluation of two series of 3-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines

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dc.contributor.authorT T Lan-
dc.contributor.authorD T Anh-
dc.contributor.authorH Pham-The-
dc.contributor.authorD T M Dung-
dc.contributor.authorE J Park-
dc.contributor.authorS D Jang-
dc.contributor.authorJoo Hee Kwon-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorN T Thuan-
dc.contributor.authorS B Han-
dc.contributor.authorN H Nam-
dc.date.accessioned2020-11-05T13:11:07Z-
dc.date.available2020-11-05T13:11:07Z-
dc.date.issued2020-
dc.identifier.issn16121872-
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/23210-
dc.description.abstractTwo series of 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines were designed initially as potential acetylcholine esterase inhibitors. Biological evaluation demonstrated that N-(1-benzylpiperidin-4-yl)quinazolin-4-amines significantly inhibited AChE activity. Especially, two compounds of them were found to be the most potent with relative AChE inhibition percentages of 87 % in comparison to donepezil. The docking studies with AChE showed similar interactions between donepezil and four derivatives. N-(1-Benzylpiperidin-4-yl)quinazolin-4-amines also exhibited significant DPPH scavenging effects. The two series of compound also exerted moderate to good cytotoxicity against three human cancer cell lines, including SW620 (human colon cancer), PC-3 (prostate cancer), and NCI-H23 (lung cancer), with 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one being the most cytotoxic agent. 3-[(1-Benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one significantly induced early apoptosis and arrested the SW620 cells at G2/M phase. From this study, two compounds of N-(1-benzylpiperidin-4-yl)quinazolin-4-amines could serve as new leads for further design and AChE inhibitors, while 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one could serve as a new lead for the design and development of more potent anticancer agents.-
dc.publisherWiley-
dc.titleDesign, synthesis and bioevaluation of two series of 3-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines-
dc.title.alternativeDesign, synthesis and bioevaluation of two series of 3-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines-
dc.typeArticle-
dc.citation.titleChemistry & Biodiversity-
dc.citation.number7-
dc.citation.endPagee2000290-
dc.citation.startPagee2000290-
dc.citation.volume17-
dc.contributor.affiliatedAuthorJoo Hee Kwon-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeNameLan-
dc.contributor.alternativeNameAnh-
dc.contributor.alternativeNamePham-The-
dc.contributor.alternativeNameDung-
dc.contributor.alternativeName박은재-
dc.contributor.alternativeName장선동-
dc.contributor.alternativeName권주희-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeNameThuan-
dc.contributor.alternativeName한상배-
dc.contributor.alternativeNameNam-
dc.identifier.bibliographicCitationChemistry & Biodiversity, vol. 17, no. 7, pp. e2000290-e2000290-
dc.identifier.doi10.1002/cbdv.202000290-
dc.subject.keywordacetylcholine esterase inhibitors-
dc.subject.keywordquinazolin-4(3H)-one-
dc.subject.keywordquinazolin-4-amine-
dc.subject.keywordcytotoxicity-
dc.subject.keyworddocking simulation-
dc.subject.localacetylcholine esterase inhibitors-
dc.subject.localAcetylcholine esterase inhibitors-
dc.subject.localquinazolin-4(3H)-one-
dc.subject.localQuinazolin-4(3H)-one-
dc.subject.localquinazolin-4-amine-
dc.subject.localcytotoxicity-
dc.subject.localCytotoxicity-
dc.subject.localdocking simulation-
dc.subject.localDocking simulation-
dc.description.journalClassY-
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Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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