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Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: hekmat nejad m. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S. Nishiguchi GA, et al. Among authors: hekmat nejad m. J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8. J Med Chem. 2017. PMID: 28557458
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD. Shao W, et al. Among authors: hekmat nejad m. Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17. Cancer Res. 2018. PMID: 29343524
RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation.
Holderfield M, Merritt H, Chan J, Wallroth M, Tandeske L, Zhai H, Tellew J, Hardy S, Hekmat-Nejad M, Stuart DD, McCormick F, Nagel TE. Holderfield M, et al. Among authors: hekmat nejad m. Cancer Cell. 2013 May 13;23(5):594-602. doi: 10.1016/j.ccr.2013.03.033. Cancer Cell. 2013. PMID: 23680146 Free article.
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
de Vicente J, Lemoine R, Bartlett M, Hermann JC, Hekmat-Nejad M, Henningsen R, Jin S, Kuglstatter A, Li H, Lovey AJ, Menke J, Niu L, Patel V, Petersen A, Setti L, Shao A, Tivitmahaisoon P, Vu MD, Soth M. de Vicente J, et al. Among authors: hekmat nejad m. Bioorg Med Chem Lett. 2014 Nov 1;24(21):4969-75. doi: 10.1016/j.bmcl.2014.09.031. Epub 2014 Sep 21. Bioorg Med Chem Lett. 2014. PMID: 25262541
Inhibition of prenylated KRAS in a lipid environment.
Jansen JM, Wartchow C, Jahnke W, Fong S, Tsang T, Pfister K, Zavorotinskaya T, Bussiere D, Cheng JM, Crawford K, Dai Y, Dove J, Fang E, Feng Y, Florent JM, Fuller J, Gossert AD, Hekmat-Nejad M, Henry C, Klopp J, Lenahan WP, Lingel A, Ma S, Meyer A, Mishina Y, Narberes J, Pardee G, Ramurthy S, Rieffel S, Stuart D, Subramanian S, Tandeske L, Widger S, Widmer A, Winterhalter A, Zaror I, Hardy S. Jansen JM, et al. Among authors: hekmat nejad m. PLoS One. 2017 Apr 6;12(4):e0174706. doi: 10.1371/journal.pone.0174706. eCollection 2017. PLoS One. 2017. PMID: 28384226 Free PMC article.
3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S, He Y, Hekmat-Nejad M, Hendricks T, Henningsen R, Hilgenkamp R, Ho H, Hoffman A, Hsu PY, Hu DQ, Itano A, Jaime-Figueroa S, Jahangir A, Jin S, Kuglstatter A, Kutach AK, Liao C, Lynch S, Menke J, Niu L, Patel V, Railkar A, Roy D, Shao A, Shaw D, Steiner S, Sun Y, Tan SL, Wang S, Vu MD. Soth M, et al. Among authors: hekmat nejad m. J Med Chem. 2013 Jan 10;56(1):345-56. doi: 10.1021/jm301646k. Epub 2012 Dec 19. J Med Chem. 2013. PMID: 23214979
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