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Page 1
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: setti l. 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
Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM. Jain R, et al. Among authors: setti l. J Med Chem. 2015 Sep 10;58(17):6766-83. doi: 10.1021/acs.jmedchem.5b00450. Epub 2015 Aug 13. J Med Chem. 2015. PMID: 26270416
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: setti l. 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
Design and synthesis of potent RSK inhibitors.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Appleton BA, Lindvall M, Shafer CM. Jain R, et al. Among authors: setti l. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3197-3201. doi: 10.1016/j.bmcl.2018.08.020. Epub 2018 Aug 21. Bioorg Med Chem Lett. 2018. PMID: 30170943
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Costales A, Mathur M, Ramurthy S, Lan J, Subramanian S, Jain R, Atallah G, Setti L, Lindvall M, Appleton BA, Ornelas E, Feucht P, Warne B, Doyle L, Basham SE, Aronchik I, Jefferson AB, Shafer CM. Costales A, et al. Among authors: setti l. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30. Bioorg Med Chem Lett. 2014. PMID: 24534486
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Barsanti PA, Pan Y, Lu Y, Jain R, Cox M, Aversa RJ, Dillon MP, Elling R, Hu C, Jin X, Knapp M, Lan J, Ramurthy S, Rudewicz P, Setti L, Subramanian S, Mathur M, Taricani L, Thomas G, Xiao L, Yue Q. Barsanti PA, et al. Among authors: setti l. ACS Med Chem Lett. 2014 Oct 30;6(1):42-6. doi: 10.1021/ml500352s. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589928 Free PMC 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: setti l. 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
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.
Lemoine RC, Petersen AC, Setti L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein D. Lemoine RC, et al. Among authors: setti l. Bioorg Med Chem Lett. 2010 Jan 15;20(2):704-8. doi: 10.1016/j.bmcl.2009.11.072. Epub 2009 Dec 7. Bioorg Med Chem Lett. 2010. PMID: 20004099
Spiropiperidine CCR5 antagonists.
Rotstein DM, Gabriel SD, Makra F, Filonova L, Gleason S, Brotherton-Pleiss C, Setti LQ, Trejo-Martin A, Lee EK, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Weller P, Mau CI. Rotstein DM, et al. Among authors: setti lq. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5401-6. doi: 10.1016/j.bmcl.2009.07.122. Epub 2009 Jul 30. Bioorg Med Chem Lett. 2009. PMID: 19674898
70 results