3iok Citations

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.

Abstract

Constitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.

Reviews - 3iok mentioned but not cited (1)

  1. The use of structural biology in Janus kinase targeted drug discovery. Alicea-Velázquez NL, Boggon TJ. Curr Drug Targets 12 546-555 (2011)

Articles - 3iok mentioned but not cited (2)

  1. Hit identification of IKKβ natural product inhibitor. Leung CH, Chan DS, Li YW, Fong WF, Ma DL. BMC Pharmacol Toxicol 14 3 (2013)
  2. Alchemical Grid Dock (AlGDock) calculations in the D3R Grand Challenge 3 : Binding free energies between flexible ligands and rigid receptors. Xie B, Minh DDL. J. Comput. Aided Mol. Des. 33 61-69 (2019)


Reviews citing this publication (4)

  1. The recent medicinal chemistry development of Jak2 tyrosine kinase small molecule inhibitors. Baskin R, Majumder A, Sayeski PP. Curr. Med. Chem. 17 4551-4558 (2010)
  2. Recent developments on JAK2 inhibitors: a patent review. Kiss R, Sayeski PP, Keserũ GM. Expert Opin Ther Pat 20 471-495 (2010)
  3. Progress toward JAK1-selective inhibitors. Menet CJ, Mammoliti O, López-Ramos M. Future Med Chem 7 203-235 (2015)
  4. New Strategies in Myeloproliferative Neoplasms: The Evolving Genetic and Therapeutic Landscape. Patel AB, Vellore NA, Deininger MW. Clin. Cancer Res. 22 1037-1047 (2016)

Articles citing this publication (3)

  1. Synthesis of 4-substituted pyrazole-3,5-diamines via Suzuki-Miyaura coupling and iron-catalyzed reduction. Tomanová M, Jedinák L, Košař J, Kvapil L, Hradil P, Cankař P. Org. Biomol. Chem. 15 10200-10211 (2017)
  2. A Novel Selective JAK2 Inhibitor Identified Using Pharmacological Interactions. Lin TE, HuangFu WC, Chao MW, Sung TY, Chang CD, Chen YY, Hsieh JH, Tu HJ, Huang HL, Pan SL, Hsu KC. Front Pharmacol 9 1379 (2018)
  3. A computationally affordable approach for accurate prediction of the binding affinity of JAK2 inhibitors. Mai NT, Lan NT, Vu TY, Tung NT, Phung HTT. J Mol Model 28 163 (2022)