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Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Pelz NF, Bian Z, Zhao B, Shaw S, Tarr JC, Belmar J, Gregg C, Camper DV, Goodwin CM, Arnold AL, Sensintaffar JL, Friberg A, Rossanese OW, Lee T, Olejniczak ET, Fesik SW. Pelz NF, et al. Among authors: arnold al. J Med Chem. 2016 Mar 10;59(5):2054-66. doi: 10.1021/acs.jmedchem.5b01660. Epub 2016 Feb 24. J Med Chem. 2016. PMID: 26878343 Free PMC article.
Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.
Lee T, Bian Z, Zhao B, Hogdal LJ, Sensintaffar JL, Goodwin CM, Belmar J, Shaw S, Tarr JC, Veerasamy N, Matulis SM, Koss B, Fischer MA, Arnold AL, Camper DV, Browning CF, Rossanese OW, Budhraja A, Opferman J, Boise LH, Savona MR, Letai A, Olejniczak ET, Fesik SW. Lee T, et al. Among authors: arnold al. FEBS Lett. 2017 Jan;591(1):240-251. doi: 10.1002/1873-3468.12497. Epub 2016 Dec 19. FEBS Lett. 2017. PMID: 27878989 Free PMC article.
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Shaw S, Bian Z, Zhao B, Tarr JC, Veerasamy N, Jeon KO, Belmar J, Arnold AL, Fogarty SA, Perry E, Sensintaffar JL, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW. Shaw S, et al. Among authors: arnold al. J Med Chem. 2018 Mar 22;61(6):2410-2421. doi: 10.1021/acs.jmedchem.7b01155. Epub 2018 Mar 9. J Med Chem. 2018. PMID: 29323899
Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS.
Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW. Hodges TR, et al. Among authors: arnold al. J Med Chem. 2018 Oct 11;61(19):8875-8894. doi: 10.1021/acs.jmedchem.8b01108. Epub 2018 Sep 28. J Med Chem. 2018. PMID: 30205005 Free PMC article.
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW. Lee T, et al. Among authors: arnold al. J Med Chem. 2019 Apr 25;62(8):3971-3988. doi: 10.1021/acs.jmedchem.8b01991. Epub 2019 Apr 16. J Med Chem. 2019. PMID: 30929420
Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors.
Tarr JC, Salovich JM, Aichinger M, Jeon K, Veerasamy N, Sensintaffar JL, Arnhof H, Samwer M, Christov PP, Kim K, Wunberg T, Schweifer N, Trapani F, Arnold A, Martin F, Zhao B, Miriyala N, Sgubin D, Fogarty S, Moore WJ, Stott GM, Olejniczak ET, Engelhardt H, Rudolph D, Lee T, McConnell DB, Fesik SW. Tarr JC, et al. J Med Chem. 2024 Aug 22;67(16):14370-14393. doi: 10.1021/acs.jmedchem.4c01188. Epub 2024 Aug 5. J Med Chem. 2024. PMID: 39102508 Free PMC article.
47 results