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Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.

Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W
Bioorg Med Chem Lett 18 5648-52 (2008)
Related entries: 3dbc, 3dbe, 3dbf

Cited: 9 times
EuropePMC logo PMID: 18793847

Abstract

A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of treated cells is consistent with Plk1 inhibition. A co-crystal structure of one of these compounds with zPlk1 confirms an ATP-competitive binding mode.

Reviews - 3dbd mentioned but not cited (1)

  1. Synthetic and Medicinal Chemistry Approaches Toward WEE1 Kinase Inhibitors and Its Degraders. Alli VJ, Yadav P, Suresh V, Jadav SS. ACS Omega 8 20196-20233 (2023)


Reviews citing this publication (2)

  1. Plk1-targeted small molecule inhibitors: molecular basis for their potency and specificity. Murugan RN, Park JE, Kim EH, Shin SY, Cheong C, Lee KS, Bang JK. Mol Cells 32 209-220 (2011)
  2. PLK-1 Targeted Inhibitors and Their Potential against Tumorigenesis. Kumar S, Kim J. Biomed Res Int 2015 705745 (2015)

Articles citing this publication (6)

  1. A pan-specific inhibitor of the polo-box domains of polo-like kinases arrests cancer cells in mitosis. Reindl W, Yuan J, Krämer A, Strebhardt K, Berg T. Chembiochem 10 1145-1148 (2009)
  2. Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors. Sato Y, Onozaki Y, Sugimoto T, Kurihara H, Kamijo K, Kadowaki C, Tsujino T, Watanabe A, Otsuki S, Mitsuya M, Iida M, Haze K, Machida T, Nakatsuru Y, Komatani H, Kotani H, Iwasawa Y. Bioorg Med Chem Lett 19 4673-4678 (2009)
  3. Preparation of orthogonally protected (2S, 3R)-2-amino-3-methyl-4-phosphonobutyric acid (Pmab) as a phosphatase-stable phosphothreonine mimetic and its use in the synthesis of Polo-box domain-binding peptides. Liu F, Park JE, Lee KS, Burke TR. Tetrahedron 65 9673-9679 (2009)
  4. Genetic approach to evaluate specificity of small molecule drug candidates inhibiting PLK1 using zebrafish. Zhong H, Xin S, Zhao Y, Lu J, Li S, Gong J, Yang Z, Lin S. Mol Biosyst 6 1463-1468 (2010)
  5. Synthesis and bioactivity of novel amino-pyrazolopyridines. Orlikova B, Chaouni W, Schumacher M, Aadil M, Diederich M, Kirsch G. Eur J Med Chem 85 450-457 (2014)
  6. Drug Design for ALK-Positive NSCLC: an Integrated Pharmacophore-Based 3D QSAR and Virtual Screening Strategy. James N, Shanthi V, Ramanathan K. Appl Biochem Biotechnol 185 289-315 (2018)


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