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DC Field | Value | Language |
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dc.contributor.author | Panathur, N. | - |
dc.contributor.author | Gokhale, N. | - |
dc.contributor.author | Udayakumar, D. | - |
dc.contributor.author | Koushik, P.V. | - |
dc.contributor.author | Yogeeswari, P. | - |
dc.contributor.author | Sriram, D. | - |
dc.date.accessioned | 2020-03-31T08:45:30Z | - |
dc.date.available | 2020-03-31T08:45:30Z | - |
dc.date.issued | 2016 | - |
dc.identifier.citation | Medicinal Chemistry Research, 2016, Vol.25, 1, pp.135-148 | en_US |
dc.identifier.uri | https://idr.nitk.ac.in/jspui/handle/123456789/13269 | - |
dc.description.abstract | A series of pyridazino[4,5-b]indole derivatives containing alkyl-, benzyl- and phenacyl-substituted 1,2,3-triazolylmethyl units was synthesized using click chemistry approach. All 30 compounds of the series were screened in vitro against four cancer cell lines, viz. breast cancer cells MDA-MB-231 and MCF 7, human primary glioblastoma U-87 and human neuroblastoma IMR-32 cell lines. Most of the compounds exhibited potent cancer cell growth inhibition activity at very low micromolar concentrations. The IC50 value of compounds 7v and 7x against human neuroblastoma IMR-32 cell line is 0.07 and 0.04 ?M, respectively. Among the tested compounds, ten compounds showed IC50 value less than 1 ?M against MDA-MB-231 cells, whereas against IMR-32 cells, nine compounds and, against U-87 cells, six compounds showed similar inhibition activity. Further, these molecules exhibited prominent binding affinity and docking scores in the molecular simulation study with the target enzyme PI3 kinase. Graphical Abstract: This paper illustrates the synthesis of new fused indole-pyridazinone derivatives containing substituted 1,2,3-triazoles via click chemistry approach. Most of the compounds exhibited potent cancer cell growth inhibition activity at very low micromolar concentrations. [Figure not available: see fulltext.] 2015 Springer Science+Business Media New York. | en_US |
dc.title | Synthesis of novel 5-[(1,2,3-triazol-4-yl)methyl]-1-methyl-3H-pyridazino[4,5-b]indol-4-one derivatives by click reaction and exploration of their anticancer activity | en_US |
dc.type | Article | en_US |
Appears in Collections: | 1. Journal Articles |
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