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DC Field | Value | Language |
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dc.contributor.author | Joshi, Mayank | - |
dc.contributor.author | Choudhury, Angshuman Roy | - |
dc.date.accessioned | 2023-08-21T16:05:43Z | - |
dc.date.available | 2023-08-21T16:05:43Z | - |
dc.date.issued | 2022 | - |
dc.identifier.citation | Bioorganic and Medicinal Chemistry, 67(1), 116835. | en_US |
dc.identifier.uri | https://doi.org/10.1016/j.bmc.2022.116835 | - |
dc.identifier.uri | http://hdl.handle.net/123456789/4992 | - |
dc.description | Only IISER Mohali authors are available in the record. | en_US |
dc.description.abstract | A strategy of “Nature-to-new” with iterative scaffold-hopping was considered for investigation of privileged ring/functional motif-elaborated analogs of natural aurones. An organocatalyzed umpolung chemistry based method was established for molecular-diversity feasible synthesis of title class of chemotypes i.e. (Z)-2-Arylideneimidazo[1,2–a]pyridinones and (Z)-2-Arylidenebenzo[d]imidazo[2,1–b]thiazol-3-ones. Various biophysical experiments indicated their important biological properties. The analogs showed characteristic anticancer activities with efficiency more than an anticancer drug. The compounds induced apoptosis with arrest in the S phase of the cell cycle regulation. The compounds’ significant effect in up/down-regulation of various apoptotic proteins, an apoptosis cascade, and the inhibition of topoisomerases-mediated DNA relaxation process was identified. The analysis of the structure-activity relationship, interference with biological events and the drug-likeness physicochemical properties of the compounds in the acceptable window indicated distinctive medicinal molecule-to-properties of the investigated chemotypes. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Organocatalyzed umpolung | en_US |
dc.subject | synthesis of heterocyclic-fused | en_US |
dc.subject | arylidene-imidazolones as anticancer agents | en_US |
dc.title | Organocatalyzed umpolung addition for synthesis of heterocyclic-fused arylidene-imidazolones as anticancer agents | en_US |
dc.type | Article | en_US |
Appears in Collections: | Research Articles |
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