DC Field | Value | Language |
---|---|---|
dc.contributor.author | T T Lan | - |
dc.contributor.author | D T Anh | - |
dc.contributor.author | H Pham-The | - |
dc.contributor.author | D T M Dung | - |
dc.contributor.author | E J Park | - |
dc.contributor.author | S D Jang | - |
dc.contributor.author | Joo Hee Kwon | - |
dc.contributor.author | Jong Soon Kang | - |
dc.contributor.author | N T Thuan | - |
dc.contributor.author | S B Han | - |
dc.contributor.author | N H Nam | - |
dc.date.accessioned | 2020-11-05T13:11:07Z | - |
dc.date.available | 2020-11-05T13:11:07Z | - |
dc.date.issued | 2020 | - |
dc.identifier.issn | 1612-1872 | - |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/23210 | - |
dc.description.abstract | 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 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.publisher | Wiley | - |
dc.title | 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 | - |
dc.title.alternative | 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 | - |
dc.type | Article | - |
dc.citation.title | Chemistry & Biodiversity | - |
dc.citation.number | 7 | - |
dc.citation.endPage | e2000290 | - |
dc.citation.startPage | e2000290 | - |
dc.citation.volume | 17 | - |
dc.contributor.affiliatedAuthor | Joo Hee Kwon | - |
dc.contributor.affiliatedAuthor | Jong Soon Kang | - |
dc.contributor.alternativeName | Lan | - |
dc.contributor.alternativeName | Anh | - |
dc.contributor.alternativeName | Pham-The | - |
dc.contributor.alternativeName | Dung | - |
dc.contributor.alternativeName | 박은재 | - |
dc.contributor.alternativeName | 장선동 | - |
dc.contributor.alternativeName | 권주희 | - |
dc.contributor.alternativeName | 강종순 | - |
dc.contributor.alternativeName | Thuan | - |
dc.contributor.alternativeName | 한상배 | - |
dc.contributor.alternativeName | Nam | - |
dc.identifier.bibliographicCitation | Chemistry & Biodiversity, vol. 17, no. 7, pp. e2000290-e2000290 | - |
dc.identifier.doi | 10.1002/cbdv.202000290 | - |
dc.subject.keyword | acetylcholine esterase inhibitors | - |
dc.subject.keyword | quinazolin-4(3H)-one | - |
dc.subject.keyword | quinazolin-4-amine | - |
dc.subject.keyword | cytotoxicity | - |
dc.subject.keyword | docking simulation | - |
dc.subject.local | acetylcholine esterase inhibitors | - |
dc.subject.local | Acetylcholine esterase inhibitors | - |
dc.subject.local | Quinazolin-4(3H)-one | - |
dc.subject.local | Quinazolin?4(3H)?one | - |
dc.subject.local | quinazolin-4(3H)-one | - |
dc.subject.local | quinazolin-4-amine | - |
dc.subject.local | Cytotoxicity | - |
dc.subject.local | cytotoxicity | - |
dc.subject.local | Docking simulation | - |
dc.subject.local | Docking simulations | - |
dc.subject.local | docking simulation | - |
dc.description.journalClass | Y | - |
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