Development of ortho-Chlorophenyl Substituted Pyrimidines as Exceptionally Potent Aurora Kinase Inhibitors

The ortho-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC(50) = 6.1 ± 1.0 nM) from in-house screening. Detailed structure activity relationship (SAR) studies indicated that polar substituents at the para position of the B-ring are critical for potent ac...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Lawrence, Harshani R., Martin, Matthew P., Luo, Yunting, Pireddu, Roberta, Yang, Hua, Gevariya, Harsukh, Ozcan, Sevil, Zhu, Jin-Yi, Kendig, Robert, Rodriguez, Mercedes, Elias, Roy, Cheng, Jin Q., Sebti, Saïd M., Schonbrunn, Ernst, Lawrence, Nicholas J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4429609/
https://ncbi.nlm.nih.gov/pubmed/22803810
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300334d
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