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Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.

Huestis MP, Dela Cruz D, DiPasquale AG, Durk MR, Eigenbrot C, Gibbons P, Gobbi A, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Siu M, Rudolph J
J Med Chem 64 3940-3955 (2021)
Cited: 6 times
EuropePMC logo PMID: 33780623

Abstract

Optimization of a series of aryl urea RAF inhibitors led to the identification of type II pan-RAF inhibitor GNE-0749 (

Articles - 6xlo mentioned but not cited (1)

  1. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor. Huestis MP, Durk MR, Eigenbrot C, Gibbons P, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Rudolph J, Siu M. ACS Med Chem Lett 12 791-797 (2021)


Reviews citing this publication (2)

  1. Selected Approaches to Disrupting Protein-Protein Interactions within the MAPK/RAS Pathway. Harwood SJ, Smith CR, Lawson JD, Ketcham JM. Int J Mol Sci 24 7373 (2023)
  2. Targeting CRAF kinase in anti-cancer therapy: progress and opportunities. Wang P, Laster K, Jia X, Dong Z, Liu K. Mol Cancer 22 208 (2023)

Articles citing this publication (3)

  1. Discovery of New Quinolone-Based Diarylamides as Potent B-RAFV600E/C-RAF Kinase Inhibitors Endowed with Promising In Vitro Anticancer Activity. Kim HJ, Park JW, Seo S, Cho KH, Alanazi MM, Bang EK, Keum G, El-Damasy AK. Int J Mol Sci 24 3216 (2023)
  2. Phenyloxycarbonyl (Phoc) Carbamate: Chemioselective Reactivity and Tetra-n-butylammonium Fluoride Deprotection Study. Huguenot F, Vidal M. ACS Omega 7 44861-44868 (2022)
  3. Targeting RAF Isoforms and Tumor Microenvironments in RAS or BRAF Mutant Colorectal Cancers with SJ-C1044 for Anti-Tumor Activity. Hong S, Jeon M, Kwon J, Park H, Lee G, Kim K, Ahn S. Curr Issues Mol Biol 45 5865-5878 (2023)


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