4hyu › Citations

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.

Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY
Bioorg Med Chem Lett 23 1486-92 (2013)
Cited: 10 times
EuropePMC logo PMID: 23352510

Abstract

A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC(50)=16 and 66 nM, respectively), with bioavailability in rats and suitable for further in vivo pharmacological evaluation.

Reviews - 4hyu mentioned but not cited (1)

  1. C-Jun N-terminal kinase inhibitors: Structural insight into kinase-inhibitor complexes. Duong MTH, Lee JH, Ahn HC. Comput Struct Biotechnol J 18 1440-1457 (2020)

Articles - 4hyu mentioned but not cited (3)

  1. Isorhamnetin inhibits amplification of influenza A H1N1 virus inflammation mediated by interferon via the RIG-I/JNK pathway. Li J, Xu Y, Lin Z, Guan L, Chen S, Zhou L. Ann Transl Med 9 1327 (2021)
  2. Discovery of Pyrimidine- and Coumarin-Linked Hybrid Molecules as Inducers of JNK Phosphorylation through ROS Generation in Breast Cancer Cells. Kim NY, Vishwanath D, Xi Z, Nagaraja O, Swamynayaka A, Kumar Harish K, Basappa S, Madegowda M, Pandey V, Sethi G, Lobie PE, Ahn KS, Basappa B. Molecules 28 3450 (2023)
  3. Proposing the Promiscuous Protein Structures in JNK1 and JNK3 for Virtual Screening in Pursuit of Potential Leads. Sailapathi A, Murugan G, Somarathinam K, Gunalan S, Jagadeesan R, Yoosuf N, Kanagaraj S, Kothandan G. ACS Omega 5 3969-3978 (2020)


Reviews citing this publication (1)

  1. c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014). Gehringer M, Muth F, Koch P, Laufer SA. Expert Opin Ther Pat 25 849-872 (2015)

Articles citing this publication (5)

  1. Are there physicochemical differences between allosteric and competitive ligands? Smith RD, Lu J, Carlson HA. PLoS Comput Biol 13 e1005813 (2017)
  2. Letter Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties. Gong L, Han X, Silva T, Tan YC, Goyal B, Tivitmahaisoon P, Trejo A, Palmer W, Hogg H, Jahagir A, Alam M, Wagner P, Stein K, Filonova L, Loe B, Makra F, Rotstein D, Rapatova L, Dunn J, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Hermann J, Kuglstatter A, Goldstein D. Bioorg Med Chem Lett 23 3565-3569 (2013)
  3. Pyrazole derivatives as potent inhibitors of c-Jun N-terminal kinase: synthesis and SAR studies. Doma A, Kulkarni R, Palakodety R, Sastry GN, Sridhara J, Garlapati A. Bioorg Med Chem 22 6209-6219 (2014)
  4. An image-based Pathogen Box screen identifies new compounds with anti-Giardia activity and highlights the importance of assay choice in phenotypic drug discovery. Tiash S, Saunders J, Hart CJS, Ryan JH, Riches AG, Skinner-Adams TS. Int J Parasitol Drugs Drug Resist 12 60-67 (2020)
  5. The Disappearing Director: The Case of Directed N-Arylation via a Removable Hydroxyl Group. Andrzejewska MR, Vuram PK, Pottabathini N, Gurram V, Relangi SS, Korvinson KA, Doddipalla R, Stahl L, Neary MC, Pradhan P, Sharma S, Lakshman MK. Adv Synth Catal 360 2503-2510 (2018)


Quick links