The Synthesis and Biological Evaluation of Some C-9 and C-10 Substituted Derivatives of the RNA Polymerase I Transcription Inhibitor CX-5461
- Author(s)
- Amarasiri, M; Vo, Y; Gardiner, MG; Poh, P; Soo, P; Pavy, M; Hein, N; Ferreira, R; Hannan, KM; Hannan, RD; Banwell, MG;
- Details
- Publication Year 2021,Volume 74,Issue #7,Page 540-556
- Journal Title
- Australian Journal of Chemistry
- Publication Type
- Research article
- Abstract
- The regio-isomeric alkynyl-substituted derivatives, 2 and 3, of the RNA Polymerase I (Pol I) transcription inhibitor CX-5461 (1) were prepared and the active one (compound 3) subjected to click reactions ([3 + 2]-cycloaddition reactions) with certain alkyl azides bearing biotin or fluorescent tags. Compounds 2 and 3, as well as four [3 + 2]-cycloadducts of the latter, were subjected to biological evaluation in a human acute myeloid leukemia cell line model. Among the six compounds tested only alkyne 3 remained active but this was less potent than parent 1.
- Keywords
- alkyne; azide; biotin; cancer; click chemistry; fluorescent; ribosomal RNA; RNA Polymerase 1 inhibitor; synthesis; tagging
- Department(s)
- Laboratory Research
- Publisher's Version
- https://doi.org/10.1071/CH21049
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2025-05-23 04:02:57
Last Modified: 2025-05-23 04:04:10