Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 남태규 | - |
dc.date.accessioned | 2019-01-25T07:19:39Z | - |
dc.date.available | 2019-01-25T07:19:39Z | - |
dc.date.issued | 2018-10 | - |
dc.identifier.citation | CHEMICO-BIOLOGICAL INTERACTIONS, v. 294, Page. 1-8 | en_US |
dc.identifier.issn | 0009-2797 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0009279718306641 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/81446 | - |
dc.description.abstract | Enhanced expression of NADPH oxidase (NOX) and the subsequent production of reactive oxygen species (ROS) are associated with lung cancer. In the present study, fifty 6-amino-2,4,5-trimethylpyridin-3-ol derivatives were screened for anticancer activity by targeting NOX2-derived ROS. The compounds suppressed ROS production and decreased cancer cell viability (R-2= 0.79). Among the derivatives, the compound coded BJ-1207, which contained a 4-(hydroxydiphenylmethyl) piperidine moiety, exhibited the most effective anticancer activity against A549 lung cancer cell line and eight other cancer cell lines, including H1299, MCF-7, MDA-MB-231, HT29, SW620, Mia PaCa-2, PANC-1, and U937. BJ-1207 also showed significantly lower inhibitory effects on kinase insert domain receptor (KDR) and c-KIT tyrosine kinase but higher inhibitory activity on NOX than those of sunitinib, a multi-receptor tyrosine kinase (RTK) inhibitor. In addition, BJ-1207-induced inhibition of RTK-downstream signaling pathways, such as ROS production, and expression of target genes, such as stem cell factor and transforming growth factor-alpha, were similar to those induced by sunitinib. In the xenograft chick tumor model, BJ-1207 inhibited lung tumor growth to a similar or much greater extent than that of sunitinib or cisplatin, respectively. Overall, the present study showed that BJ-1207, a vitamin B-6-derived 2,4,5-trimethylpyridin-3-ol compound with azacyclonol moiety at C (6)-position of the pyridine ring, inhibited NOX activity and that it is a promising lead compound for developing anticancer drugs against lung cancer. | en_US |
dc.description.sponsorship | This work was supported by the Yeungnam University Research Grant. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | ELSEVIER IRELAND LTD | en_US |
dc.subject | Aminopyridin-3-ols | en_US |
dc.subject | Non-small cell lung cancer | en_US |
dc.subject | NADPH oxidase | en_US |
dc.subject | Stem cell factor | en_US |
dc.subject | Transforming growth factor-alpha | en_US |
dc.title | Antitumor activity of BJ-1207, a 6-amino-2,4,5-trimethylpyridin-3-ol derivative, in human lung cancer | en_US |
dc.type | Article | en_US |
dc.relation.volume | 294 | - |
dc.identifier.doi | 10.1016/j.cbi.2018.08.007 | - |
dc.relation.page | 1-8 | - |
dc.relation.journal | CHEMICO-BIOLOGICAL INTERACTIONS | - |
dc.contributor.googleauthor | Gautam, Jaya | - |
dc.contributor.googleauthor | Banskota, Suhrid | - |
dc.contributor.googleauthor | Chaudhary, Prakash | - |
dc.contributor.googleauthor | Dahal, Sadan | - |
dc.contributor.googleauthor | Kim, Dong-Guk | - |
dc.contributor.googleauthor | Kang, Han-eol | - |
dc.contributor.googleauthor | Lee, Iyn-Hyang | - |
dc.contributor.googleauthor | Nam, Tae-Gyu | - |
dc.contributor.googleauthor | Jeong, Byeong-Seon | - |
dc.contributor.googleauthor | Kim, Jung-Ae | - |
dc.relation.code | 2018001480 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | tnam | - |
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