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Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.

Esvan YJ, Zeinyeh W, Boibessot T, Nauton L, Théry V, Knapp S, Chaikuad A, Loaëc N, Meijer L, Anizon F, Giraud F, Moreau P
Eur J Med Chem 118 170-7 (2016)
Cited: 9 times
EuropePMC logo PMID: 27128181

Abstract

The design and synthesis of new pyrido[3,4-g]quinazoline derivatives is described as well as their protein kinase inhibitory potencies toward five CMGC family members (CDK5, CK1, GSK3, CLK1 and DYRK1A). The interest for this original tricyclic heteroaromatic scaffold as modulators of CLK1/DYRK1A activity was validated by nanomolar potencies (compounds 12 and 13). CLK1 co-crystal structures with two inhibitors revealed the binding mode of these compounds within the ATP-binding pocket.

Reviews - 5j1w mentioned but not cited (1)

  1. Dual-Specificity, Tyrosine Phosphorylation-Regulated Kinases (DYRKs) and cdc2-Like Kinases (CLKs) in Human Disease, an Overview. Lindberg MF, Meijer L. Int J Mol Sci 22 6047 (2021)


Articles citing this publication (8)

  1. Indole-3-Carbonitriles as DYRK1A Inhibitors by Fragment-Based Drug Design. Meine R, Becker W, Falke H, Preu L, Loaëc N, Meijer L, Kunick C. Molecules 23 (2018)
  2. Synthesis of Bioactive 2-(Arylamino)thiazolo[5,4-f]-quinazolin-9-ones via the Hügershoff Reaction or Cu- Catalyzed Intramolecular C-S Bond Formation. Hédou D, Dubouilh-Benard C, Loaëc N, Meijer L, Fruit C, Besson T. Molecules 21 (2016)
  3. Alternative RNA splicing modulates ribosomal composition and determines the spatial phenotype of glioblastoma cells. Larionova TD, Bastola S, Aksinina TE, Anufrieva KS, Wang J, Shender VO, Andreev DE, Kovalenko TF, Arapidi GP, Shnaider PV, Kazakova AN, Latyshev YA, Tatarskiy VV, Shtil AA, Moreau P, Giraud F, Li C, Wang Y, Rubtsova MP, Dontsova OA, Condro M, Ellingson BM, Shakhparonov MI, Kornblum HI, Nakano I, Pavlyukov MS. Nat Cell Biol 24 1541-1557 (2022)
  4. 5-Methoxybenzothiophene-2-Carboxamides as Inhibitors of Clk1/4: Optimization of Selectivity and Cellular Potency. ElHady AK, El-Gamil DS, Chen PJ, Hwang TL, Abadi AH, Abdel-Halim M, Engel M. Molecules 26 1001 (2021)
  5. Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. Walter A, Chaikuad A, Helmer R, Loaëc N, Preu L, Ott I, Knapp S, Meijer L, Kunick C. PLoS ONE 13 e0196761 (2018)
  6. Synthesis and Biological Activity of Benzamides Substituted with Pyridine-Linked 1,2,4-Oxadiazole. Yang S, Tian XY, Ma TY, Dai L, Ren CL, Mei JC, Liu XH, Tan CX. Molecules 25 (2020)
  7. Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines. Defois M, Rémondin C, Josselin B, Nauton L, Théry V, Anizon F, Ruchaud S, Giraud F, Moreau P. Molecules 27 5578 (2022)
  8. [b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors. Lechner C, Flaßhoff M, Falke H, Preu L, Loaëc N, Meijer L, Knapp S, Chaikuad A, Kunick C. Molecules 24 (2019)


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