| Autor: |
Gulshan Kumar, Chinmay Das, Ayan Acharya, Subhasmita Bhal, Mayank Joshi, Chanakya Nath Kundu, Angshuman Roy Choudhury, Sankar K. Guchhait |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Bioorganicmedicinal chemistry. 67 |
| ISSN: |
1464-3391 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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