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Page 1
An orally available non-nucleotide STING agonist with antitumor activity.
Pan BS, Perera SA, Piesvaux JA, Presland JP, Schroeder GK, Cumming JN, Trotter BW, Altman MD, Buevich AV, Cash B, Cemerski S, Chang W, Chen Y, Dandliker PJ, Feng G, Haidle A, Henderson T, Jewell J, Kariv I, Knemeyer I, Kopinja J, Lacey BM, Laskey J, Lesburg CA, Liang R, Long BJ, Lu M, Ma Y, Minnihan EC, O'Donnell G, Otte R, Price L, Rakhilina L, Sauvagnat B, Sharma S, Tyagarajan S, Woo H, Wyss DF, Xu S, Bennett DJ, Addona GH. Pan BS, et al. Among authors: tyagarajan s. Science. 2020 Aug 21;369(6506):eaba6098. doi: 10.1126/science.aba6098. Science. 2020. PMID: 32820094
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: tyagarajan s. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL. Tyagarajan S, et al. Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21195616
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. Among authors: tyagarajan s. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Eid R, Fisher MH, Parsons WH, Wyvratt MJ, Lyons KA, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Weber A, Duffy JL. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. doi: 10.1016/j.bmcl.2010.10.017. Epub 2010 Oct 14. Bioorg Med Chem Lett. 2010. PMID: 21106456
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Murali Dhar TG, Nagarathnam D, Marzabadi MR, Lagu B, Wong WC, Chiu G, Tyagarajan S, Miao SW, Zhang F, Sun W, Tian D, Shen Q, Zhang J, Wetzel JM, Forray C, Chang RS, Broten TP, Schorn TW, Chen TB, O'Malley S, Ransom R, Schneck K, Bendesky R, Harrell CM, Vyas KP, et al. Murali Dhar TG, et al. Among authors: tyagarajan s. J Med Chem. 1999 Nov 18;42(23):4778-93. doi: 10.1021/jm990201h. J Med Chem. 1999. PMID: 10579841
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.
Chakravarty PK, Shih TL, Colletti SL, Ayer MB, Snedden C, Kuo H, Tyagarajan S, Gregory L, Zakson-Aiken M, Shoop WL, Schmatz DM, Wyvratt M, Fisher MH, Meinke PT. Chakravarty PK, et al. Among authors: tyagarajan s. Bioorg Med Chem Lett. 2003 Jan 6;13(1):147-50. doi: 10.1016/s0960-894x(02)00826-0. Bioorg Med Chem Lett. 2003. PMID: 12467636
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P, Harsch A, Heidebrecht R, Hughes B, Jung J, Kenific CM, Kral AM, Meinke PT, Middleton RE, Ozerova N, Sloman DL, Stanton MG, Szewczak AA, Tyagarajan S, Witter DJ, Secrist JP, Miller TA. Methot JL, et al. Among authors: tyagarajan s. Bioorg Med Chem Lett. 2008 Feb 1;18(3):973-8. doi: 10.1016/j.bmcl.2007.12.031. Epub 2008 Jan 7. Bioorg Med Chem Lett. 2008. PMID: 18182289
Substituted biaryl pyrazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5480-3. doi: 10.1016/j.bmcl.2010.07.080. Epub 2010 Jul 24. Bioorg Med Chem Lett. 2010. PMID: 20709545
69 results