ArticleTetrahedron letters2012
Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.
Article in Tetrahedron letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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Who cites it
14 citing papers in PubMed.
- Separation, Structural Elucidation, and Anticancer Activity of a Diastereoisomer of Betulonic Acid-Zidovudine Conjugates.ACS omega · 2026Article
- Molecular Diversity of Lupane Hybrids in Drug Design and Materials Science.Molecules (Basel, Switzerland) · 2025Review
- Article
- The Use of Zidovudine Pharmacophore in Multi-Target-Directed Ligands for AIDS Therapy.Molecules (Basel, Switzerland) · 2022Review
- Semisynthetic Derivatives of Pentacyclic Triterpenes Bearing Heterocyclic Moieties with Therapeutic Potential.Molecules (Basel, Switzerland) · 2022Review
- Glycoconjugation of Betulin Derivatives Using Copper-Catalyzed 1,3-Dipolar Azido-Alkyne Cycloaddition Reaction and a Preliminary Assay of Cytotoxicity of the Obtained Compounds.Molecules (Basel, Switzerland) · 2020Article
- Recent advances in natural anti-HIV triterpenoids and analogs.Medicinal research reviews · 2020Review
- Synthesis and Pharmacological Effects of Diosgenin-Betulinic Acid Conjugates.Molecules (Basel, Switzerland) · 2020Article
- Structure and Anti-HIV Activity of Betulinic Acid Analogues.Current medical science · 2018Review
- Novel Triazole Hybrids of Betulin: Synthesis and Biological Activity Profile.Molecules (Basel, Switzerland) · 2017Article
- Antineoplastic agents. 595. Structural modifications of betulin and the X-ray crystal structure of an unusual betulin amine dimer.Journal of natural products · 2014Article
- 1,2,3-triazole-substituted oleanolic Acid derivatives: synthesis and antiproliferative activity.Molecules (Basel, Switzerland) · 2013Article
- Synthesis, structure and cytotoxic activity of new acetylenic derivatives of betulin.Molecules (Basel, Switzerland) · 2013Article
- Preparation of azidoaryl- and azidoalkyloxazoles for click chemistry.Tetrahedron letters · 2012Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
In the present study, a new strategy to link AZT with betulin/betulinic acid (BA) by click chemistry was designed and achieved. This conjugation via a triazole linkage offers a new direction for modification of anti-HIV triterpenes. Click chemistry provides an easy and productive way for linking two molecules, even when one of them is a large natural product. Among the newly synthesized conjugates, compounds 15 and 16 showed potent anti-HIV activity with EC(50) values of 0.067 and 0.10 µM, respectively, which are comparable to that of AZT (EC(50): 0.10 µM) in the same assay.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.