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The design, synthesis, and biological evaluation of PIM kinase inhibitors.

Tsuhako AL, Brown DS, Koltun ES, Aay N, Arcalas A, Chan V, Du H, Engst S, Franzini M, Galan A, Huang P, Johnston S, Kane B, Kim MH, Laird AD, Lin R, Mock L, Ngan I, Pack M, Stott G, Stout TJ, Yu P, Zaharia C, Zhang W, Zhou P, Nuss JM, Kearney PC, Xu W
Bioorg Med Chem Lett 22 3732-8 (2012)
Related entries: 4alu, 4alv

Cited: 18 times
EuropePMC logo PMID: 22542012

Abstract

A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were potent, but had cell permeability limitation. Using X-ray crystal structures of the bound PIM-1 complexes with 3, 5m, and 6d, we were able to guide the SAR and identify the alkyl benzofuropyrimidinone (6l) with good PIM potencies, permeability, and oral exposure.

Reviews - 4alw mentioned but not cited (1)

  1. The Development of CK2 Inhibitors: From Traditional Pharmacology to in Silico Rational Drug Design. Cozza G. Pharmaceuticals (Basel) 10 E26 (2017)

Articles - 4alw mentioned but not cited (2)

  1. Identification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cells. Andreoli M, Persico M, Kumar A, Orteca N, Kumar V, Pepe A, Mahalingam S, Alegria AE, Petrella L, Sevciunaite L, Camperchioli A, Mariani M, Di Dato A, Novellino E, Scambia G, Malhotra SV, Ferlini C, Fattorusso C. J Med Chem 57 7916-7932 (2014)
  2. Structural analysis of PIM1 kinase complexes with ATP-competitive inhibitors. Bogusz J, Zrubek K, Rembacz KP, Grudnik P, Golik P, Romanowska M, Wladyka B, Dubin G. Sci Rep 7 13399 (2017)


Articles citing this publication (15)

  1. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Foulks JM, Carpenter KJ, Luo B, Xu Y, Senina A, Nix R, Chan A, Clifford A, Wilkes M, Vollmer D, Brenning B, Merx S, Lai S, McCullar MV, Ho KK, Albertson DJ, Call LT, Bearss JJ, Tripp S, Liu T, Stephens BJ, Mollard A, Warner SL, Bearss DJ, Kanner SB. Neoplasia 16 403-412 (2014)
  2. Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design. Wang X, Magnuson S, Pastor R, Fan E, Hu H, Tsui V, Deng W, Murray J, Steffek M, Wallweber H, Moffat J, Drummond J, Chan G, Harstad E, Ebens AJ. Bioorg Med Chem Lett 23 3149-3153 (2013)
  3. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. Sasi NK, Tiwari K, Soon FF, Bonte D, Wang T, Melcher K, Xu HE, Weinreich M. PLoS One 9 e113300 (2014)
  4. Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors. Suchaud V, Gavara L, Saugues E, Nauton L, Théry V, Anizon F, Moreau P. Bioorg Med Chem 21 4102-4111 (2013)
  5. The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors. Wang HL, Cee VJ, Chavez F, Lanman BA, Reed AB, Wu B, Guerrero N, Lipford JR, Sastri C, Winston J, Andrews KL, Huang X, Lee MR, Mohr C, Xu Y, Zhou Y, Tasker AS. Bioorg Med Chem Lett 25 834-840 (2015)
  6. Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases. Casuscelli F, Ardini E, Avanzi N, Casale E, Cervi G, D'Anello M, Donati D, Faiardi D, Ferguson RD, Fogliatto G, Galvani A, Marsiglio A, Mirizzi DG, Montemartini M, Orrenius C, Papeo G, Piutti C, Salom B, Felder ER. Bioorg Med Chem 21 7364-7380 (2013)
  7. Identification of novel inhibitors for Pim-1 kinase using pharmacophore modeling based on a novel method for selecting pharmacophore generation subsets. Shahin R, Swellmeen L, Shaheen O, Aboalhaija N, Habash M. J Comput Aided Mol Des 30 39-68 (2016)
  8. Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors. Wu B, Wang HL, Cee VJ, Lanman BA, Nixey T, Pettus L, Reed AB, Wurz RP, Guerrero N, Sastri C, Winston J, Lipford JR, Lee MR, Mohr C, Andrews KL, Tasker AS. Bioorg Med Chem Lett 25 775-780 (2015)
  9. The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors. Wurz RP, Pettus LH, Jackson C, Wu B, Wang HL, Herberich B, Cee V, Lanman BA, Reed AB, Chavez F, Nixey T, Laszlo J, Wang P, Nguyen Y, Sastri C, Guerrero N, Winston J, Lipford JR, Lee MR, Andrews KL, Mohr C, Xu Y, Zhou Y, Reid DL, Tasker AS. Bioorg Med Chem Lett 25 847-855 (2015)
  10. Understanding PIM-1 kinase inhibitor interactions with free energy simulation. Wang X, Sun Z. Phys Chem Chem Phys 21 7544-7558 (2019)
  11. Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I. Barberis C, Moorcroft N, Arendt C, Levit M, Moreno-Mazza S, Batchelor J, Mechin I, Majid T. Bioorg Med Chem Lett 27 4730-4734 (2017)
  12. Synthesis of new pyridothienopyrimidinone derivatives as Pim-1 inhibitors. Naguib BH, El-Nassan HB, Abdelghany TM. J Enzyme Inhib Med Chem 32 457-467 (2017)
  13. Synthesis of new thieno[2,3-b]pyridine derivatives as pim-1 inhibitors. Naguib BH, El-Nassan HB. J Enzyme Inhib Med Chem 31 1718-1725 (2016)
  14. Synthesis of pyrazolo[4,3-a]phenanthridines, a new scaffold for Pim kinase inhibition. Suchaud V, Gavara L, Giraud F, Nauton L, Théry V, Anizon F, Moreau P. Bioorg Med Chem 22 4704-4710 (2014)
  15. Synthesis of new pyridothienopyrimidinone and pyridothienotriazolopyrimidine derivatives as pim-1 inhibitors. El-Nassan HB, Naguib BH, Beshay EA. J Enzyme Inhib Med Chem 33 58-66 (2018)


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