Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.

Killian Oukoloff,Jane Kovalevich,Anne-Sophie Cornec,Yuemang Yao, Zachary A Owyang,Michael James,John Q Trojanowski,Virginia M-Y Lee,Amos B Smith,Kurt R Brunden,Carlo Ballatore

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•Microtubule (MT)-active triazolopyrimidines can preserve or disrupt MT integrity.•A series of photoactivatable derivatives was designed, synthesized and evaluated.•Selected photoactivatable candidate probes have been identified.•Such probes may be used in photoaffinity labeling studies.

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关键词

Triazolopyrimidine,Microtubule stabilization,Photoaffinity labeling,CNS drug discovery

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