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Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Dwyer MP, Paruch K, Labroli M, Alvarez C, Keertikar KM, Poker C, Rossman R, Fischmann TO, Duca JS, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ
Bioorg Med Chem Lett 21 467-70 (2011)
Cited: 24 times
EuropePMC logo PMID: 21094608

Abstract

The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a]pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed.

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  1. Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies. Matthews TP, Jones AM, Collins I. Expert Opin Drug Discov 8 621-640 (2013)
  2. Progress of the synthesis of condensed pyrazole derivatives (from 2010 to mid-2013). Li M, Zhao BX. Eur J Med Chem 85 311-340 (2014)
  3. An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. Cherukupalli S, Karpoormath R, Chandrasekaran B, Hampannavar GA, Thapliyal N, Palakollu VN. Eur J Med Chem 126 298-352 (2017)
  4. 5-Aminopyrazole as precursor in design and synthesis of fused pyrazoloazines. Aggarwal R, Kumar S. Beilstein J Org Chem 14 203-242 (2018)
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