ArticleBioorganic & medicinal chemistry letters2018
Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Structure-Activity Relationship and Target Investigation of Thiophen-2-yl-Pyrimidines againstbioRxiv : the preprint server for biology · 2025Article
- Photoaffinity labeling of protein targets in a complex metazoan: proof-of-concept using a probe forbioRxiv : the preprint server for biology · 2025Article
- Uncovering the Mechanism of Action of Antiprotozoal Agents: A Survey on Photoaffinity Labeling Strategy.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Design, Synthesis, and Evaluation of An Anti-trypanosomal [1,2,4]Triazolo[1,5-a]pyrimidine Probe for Photoaffinity Labeling Studies.ChemMedChem · 2024Article
- Article
- Structure-Activity Relationships, Tolerability and Efficacy of Microtubule-Active 1,2,4-Triazolo[1,5-bioRxiv : the preprint server for biology · 2023Article
- 3-Aryl-5-aminobiphenyl Substituted [1,2,4]triazolo[4,3-Molecules (Basel, Switzerland) · 2023Article
- Design, Synthesis and Biological Evaluation of [1,2,4]Triazolo[1,5-Molecules (Basel, Switzerland) · 2022Article
- Congeners Derived from Microtubule-Active Phenylpyrimidines Produce a Potent and Long-Lasting Paralysis ofACS infectious diseases · 2021Article
- Evaluation of the Structure-Activity Relationship of Microtubule-Targeting 1,2,4-Triazolo[1,5-Journal of medicinal chemistry · 2021Article
- 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.European journal of medicinal chemistry · 2019Review
- A brain-penetrant triazolopyrimidine enhances microtubule-stability, reduces axonal dysfunction and decreases tau pathology in a mouse tauopathy model.Molecular neurodegeneration · 2018Article
- Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis.ChemMedChem · 2018Article
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Authors and funding
11 authors.
Funding
Abstract
The [1,2,4]triazolo[1,5-a]pyrimidines comprise a promising class of non-naturally occurring microtubule (MT)-active compounds. Prior studies revealed that different triazolopyrimidine substitutions can yield molecules that either promote MT stabilization or disrupt MT integrity. These differences can have important ramifications in the therapeutic applications of triazolopyrimidines and suggest that different analogues may exhibit different binding modes within the same site or possibly interact with tubulin/MTs at alternative binding sites. To help discern these possibilities, a series of photoactivatable triazolopyrimidine congeners was designed, synthesized and evaluated in cellular assays with the goal of identifying candidate probes for photoaffinity labeling experiments. These studies led to the identification of different derivatives that incorporate a diazirine ring in the amine substituent at position 7 of the triazolopyrimidine heterocycle, resulting in molecules that either promote stabilization of MTs or disrupt MT integrity. These photoactivatable candidate probes hold promise to investigate the mode of action of MT-active triazolopyrimidines.
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