Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy

We report the design, synthesis, and biological evaluation of heterocyclic-fused pyrimidines as tubulin polymerization inhibitors targeting the colchicine binding site with significantly improved therapeutic index. Additionally, for the first time, we report high-resolution X-ray crystal structures...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Banerjee, Souvik, Arnst, Kinsie E., Wang, Yuxi, Kumar, Gyanendra, Deng, Shanshan, Yang, Lei, Li, Guo-bo, Yang, Jinliang, White, Stephen W., Li, Wei, Miller, Duane D.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5912893/
https://ncbi.nlm.nih.gov/pubmed/29406710
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b01858
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