ArticleMolecules (Basel, Switzerland)2014
Design and synthesis of a series of truncated neplanocin fleximers.
Article in Molecules (Basel, Switzerland), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro.Bioorganic & medicinal chemistry · 2020Article
- Nucleoside Analogs with Fleximer Nucleobase.Chemistry of heterocyclic compounds · 2020Article
- Probing the Effects of Pyrimidine Functional Group Switches on Acyclic Fleximer Analogues for Antiviral Activity.Molecules (Basel, Switzerland) · 2019Article
- The evolution of antiviral nucleoside analogues: A review for chemists and non-chemists. Part II: Complex modifications to the nucleoside scaffold.Antiviral research · 2019Review
- The evolution of nucleoside analogue antivirals: A review for chemists and non-chemists. Part 1: Early structural modifications to the nucleoside scaffold.Antiviral research · 2018Review
- Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics: synthesis and biological evaluation.Beilstein journal of organic chemistry · 2016Article
- Flexibility-Not just for yoga anymore!Antiviral chemistry & chemotherapyReview
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Authors and funding
6 authors.
Funding
Abstract
In an effort to study the effects of flexibility on enzyme recognition and activity, we have developed several different series of flexible nucleoside analogues in which the purine base is split into its respective imidazole and pyrimidine components. The focus of this particular study was to synthesize the truncated neplanocin A fleximers to investigate their potential anti-protozoan activities by inhibition of S-adenosylhomocysteine hydrolase (SAHase). The three fleximers tested displayed poor anti-trypanocidal activities, with EC50 values around 200 μM. Further studies of the corresponding ribose fleximers, most closely related to the natural nucleoside substrates, revealed low affinity for the known T. brucei nucleoside transporters P1 and P2, which may be the reason for the lack of trypanocidal activity observed.
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Registered trials
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