3kck › Citations

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.

Wang T, Ledeboer MW, Duffy JP, Salituro FG, Pierce AC, Zuccola HJ, Block E, Shlyakter D, Hogan JK, Bennani YL
Bioorg Med Chem Lett 20 153-6 (2010)
Cited: 22 times
EuropePMC logo PMID: 19945871

Abstract

Pictet-Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors.

Reviews - 3kck 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 - 3kck mentioned but not cited (8)

  1. Identification of the active substances and mechanisms of ginger for the treatment of colon cancer based on network pharmacology and molecular docking. Zhang MM, Wang D, Lu F, Zhao R, Ye X, He L, Ai L, Wu CJ. BioData Min 14 1 (2021)
  2. Fragment-Based Discovery of 6-Arylindazole JAK Inhibitors. Ritzén A, Sørensen MD, Dack KN, Greve DR, Jerre A, Carnerup MA, Rytved KA, Bagger-Bahnsen J. ACS Med Chem Lett 7 641-646 (2016)
  3. Thymoquinone Inhibits Growth of Acute Myeloid Leukemia Cells through Reversal SHP-1 and SOCS-3 Hypermethylation: In Vitro and In Silico Evaluation. Al-Rawashde FA, Johan MF, Taib WRW, Ismail I, Johari SATT, Almajali B, Al-Wajeeh AS, Nazari Vishkaei M, Al-Jamal HAN. Pharmaceuticals (Basel) 14 1287 (2021)
  4. Lipid-Based Nanoparticle Formulation of Diallyl Trisulfide Chemosensitizes the Growth Inhibitory Activity of Doxorubicin in Colorectal Cancer Model: A Novel In Vitro, In Vivo and In Silico Analysis. Alrumaihi F, Khan MA, Babiker AY, Alsaweed M, Azam F, Allemailem KS, Almatroudi AA, Ahamad SR, Alsugoor MH, Alharbi KN, Almansour NM, Khan A. Molecules 27 2192 (2022)
  5. The Effect of Liposomal Diallyl Disulfide and Oxaliplatin on Proliferation of Colorectal Cancer Cells: In Vitro and In Silico Analysis. Alrumaihi F, Khan MA, Babiker AY, Alsaweed M, Azam F, Allemailem KS, Almatroudi AA, Ahamad SR, AlSuhaymi N, Alsugoor MH, Algefary AN, Khan A. Pharmaceutics 14 236 (2022)
  6. A Novel Naphthoquinone-Coumarin Hybrid That Inhibits BCR-ABL1-STAT5 Oncogenic Pathway and Reduces Survival in Imatinib-Resistant Chronic Myelogenous Leukemia Cells. Martín-Rodríguez P, Guerra B, Hueso-Falcón I, Aranda-Tavío H, Díaz-Chico J, Quintana J, Estévez F, Díaz-Chico B, Amesty A, Estévez-Braun A, Fernández-Pérez L. Front Pharmacol 9 1546 (2018)
  7. Cheminformatics Application in the Phytochemical and Biological Study of Eucalyptus globulus L. Bark as a Potential Hepatoprotective Drug. Nematallah KA, Elmekkawy S, Abdollah MRA, Elmazar MM, Abdel-Sattar E, Abdel-Sattar E, Meselhy MR. ACS Omega 7 7945-7956 (2022)
  8. Rapid Identification of Inhibitors and Prediction of Ligand Selectivity for Multiple Proteins: Application to Protein Kinases. Ma Z, Huang SY, Cheng F, Zou X. J Phys Chem B 125 2288-2298 (2021)


Reviews citing this publication (5)

  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. The azaindole framework in the design of kinase inhibitors. Mérour JY, Buron F, Plé K, Bonnet P, Routier S. Molecules 19 19935-19979 (2014)
  3. Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors. Sharma S, Singh J, Ojha R, Singh H, Kaur M, Bedi PMS, Nepali K. Eur J Med Chem 112 298-346 (2016)
  4. Selective JAK inhibitors. Dymock BW, Yang EG, Chu-Farseeva Y, Yao L. Future Med Chem 6 1439-1471 (2014)
  5. Aldo-X Bifunctional Building Blocks for the Synthesis of Heterocycles. Ravichandiran P, Lai B, Gu Y. Chem Rec 17 142-183 (2017)

Articles citing this publication (8)

  1. Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics. Zhao H, Caflisch A. Bioorg. Med. Chem. Lett. 23 5721-5726 (2013)
  2. How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study. Kong X, Sun H, Pan P, Li D, Zhu F, Chang S, Xu L, Li Y, Hou T. Sci Rep 7 9088 (2017)
  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)
  4. A highly efficient precatalytic system (XPhos-PdG2) for the Suzuki-Miyaura cross-coupling of 7-chloro-1H-pyrrolo[2,3-c]pyridine employing low catalyst loading. Savitha B, Reddy EK, Parthasarathi D, Pakkath R, Karuvalam RP, Ananda Kumar CS, Haridas KR, Syed Ali Padusha M, Sajith AM. Mol Divers 23 697-707 (2019)
  5. Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors. Wang T, Liu X, Hao M, Qiao J, Ju C, Xue L, Zhang C. Bioorg. Med. Chem. Lett. 26 2936-2941 (2016)
  6. Ensemble docking-based virtual screening yields novel spirocyclic JAK1 inhibitors. Bajusz D, Ferenczy GG, Keserű GM. J. Mol. Graph. Model. 70 275-283 (2016)
  7. Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors. Wang Y, Huang W, Xin M, Chen P, Gui L, Zhao X, Tang F, Wang J, Liu F. Bioorg. Med. Chem. 25 75-83 (2017)
  8. The Formation of Inherently Chiral Calix[4]quinolines by Doebner-Miller Reaction of Aldehydes and Aminocalixarenes. Tlustý M, Eigner V, Dvořáková H, Lhoták P. Molecules 27 8545 (2022)


Quick links