ArticleBMC chemistry2024
Synthesis and antitumor activity of dolutegravir derivatives bearing 1,2,3-triazole moieties.
Article in BMC chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- 2Frontiers in pharmacology · 2025Article
- Synthesis of Novel Gefitinib-Conjugated 1,2,3-Triazole Derivatives and Their Effect of Inducing DNA Damage and Apoptosis in Tumor Cells.Molecules (Basel, Switzerland) · 2024Article
- Design, synthesis, and anti-inflammatory activity of 2H-1,4-benzoxazin-3(4H)-one derivatives modified with 1,2,3-triazole in LPS-induced BV-2 cells.Frontiers in pharmacology · 2024Article
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Authors and funding
9 authors.
Funding
Abstract
Modification of marketed drugs is an important way to develop drugs because its safety and clinical applicability. Oxygen-nitrogen heterocycles are a class of important active substances discovered in the process of new drug development. Dolutegravir, an HIV drug with a nitrogen-oxygen heterocycle structure, has the potential ability to inhibit cell survival. In order to find and explore novel anti-tumor drugs, new dolutegravir derivatives bearing different 1,2,3-triazole moieties were prepared via click reactions. In vitro biological experiments performed in several lung cancer cell lines suggested that these novel compounds displayed potent anti-tumor ability. Especially, the compound 9e with a substituent of 2-methyl-3-nitrophenyl and the compound 9p with a substituent of 3-trifluoromethylphenyl were effective against PC-9 cell line with IC
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