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Design, Synthesis, and Biological Activity Evaluation of Novel AZT and Adenosine-Derived 1,2,3-Triazoles
- Source :
- Journal of Chemistry, Vol 2023 (2023)
- Publication Year :
- 2023
- Publisher :
- Hindawi Limited, 2023.
-
Abstract
- CuSO4/hydrazine hydrate was used as a catalyst system for copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) of AZT and 5′-azido adenosine with terminal alkynes to give 30 novel 1,2,3-triazole derivatives. Screening for their anticancer, anti-inflammatory, angiotensin-converting enzyme 2 (ACE2), and 3C-like protease (3CLpro) inhibitory activities showed that several triazoles of AZT containing murayafoline A and indirubin-3′-oxime inhibited the growth of HepG2 and LU-1 with the IC50 values ranging from 11.01 to 19.87 μg/mL. Besides that, some triazole derivatives of adenosine exhibited anti-inflammatory activity against RAW264.7 cells with the IC50 values within an interval of 12.00–59.48.00 μg/mL. Especially, two triazoles of adenosine with indirubin-3′-oxime at O- and N1 positions expressed the ACE2 and 3CLpro inhibitory activities in which the triazole of adenosine with indirubin-3′-oxime at N1 inhibited both ACE2 and 3CLpro inhibitory activities with IC50 values of 135.62 and 142.95 μg/mL, respectively.
Details
- Language :
- English
- ISSN :
- 20909071
- Volume :
- 2023
- Database :
- Directory of Open Access Journals
- Journal :
- Journal of Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.5a1b5dd3ea3f450c89580e2d71090dd9
- Document Type :
- article
- Full Text :
- https://doi.org/10.1155/2023/1605316