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Page 1
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors.
Li D, Deng Y, Achab A, Bharathan I, Hopkins BA, Yu W, Zhang H, Sanyal S, Pu Q, Zhou H, Liu K, Lim J, Fradera X, Lesburg CA, Lammens A, Martinot TA, Cohen RD, Doty AC, Ferguson H, Nickbarg EB, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: abeywickrema p. ACS Med Chem Lett. 2021 Feb 26;12(3):389-396. doi: 10.1021/acsmedchemlett.0c00525. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738066 Free PMC article.
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.
Yu W, Deng Y, Hopkins B, Huang X, Sloman D, Zhang H, Li D, McGowan MA, White C, Pu Q, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Nickbarg EB, Cheng M, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte K, Vincent S, Sciammetta N, Bennett DJ, Han Y. Yu W, et al. Among authors: abeywickrema p. Bioorg Med Chem Lett. 2021 Sep 1;47:128214. doi: 10.1016/j.bmcl.2021.128214. Epub 2021 Jun 21. Bioorg Med Chem Lett. 2021. PMID: 34166782
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
White C, McGowan MA, Zhou H, Sciammetta N, Fradera X, Lim J, Joshi EM, Andrews C, Nickbarg EB, Cowley P, Trewick S, Augustin M, von Köenig K, Lesburg CA, Otte K, Knemeyer I, Woo H, Yu W, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Curran P, Heo MR, Abeywickrema P, Miller JR, Bennett DJ, Han Y. White C, et al. Among authors: abeywickrema p. ACS Med Chem Lett. 2020 Mar 10;11(4):550-557. doi: 10.1021/acsmedchemlett.0c00010. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292563 Free PMC article.
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Forster AB, Abeywickrema P, Bunda J, Cox CD, Cabalu TD, Egbertson M, Fay J, Getty K, Hall D, Kornienko M, Lu J, Parthasarathy G, Reid J, Sharma S, Shipe WD, Smith SM, Soisson S, Stachel SJ, Su HP, Wang D, Berger R. Forster AB, et al. Among authors: abeywickrema p. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5167-5171. doi: 10.1016/j.bmcl.2017.10.054. Epub 2017 Oct 23. Bioorg Med Chem Lett. 2017. PMID: 29113762
Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.
Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ. Raheem IT, et al. Among authors: abeywickrema p. J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26397965
Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.
Stachel SJ, Egbertson MS, Wai J, Machacek M, Toolan DM, Swestock J, Eddins DM, Puri V, McGaughey G, Su HP, Perlow D, Wang D, Ma L, Parthasarathy G, Reid JC, Abeywickrema PD, Smith SM, Uslaner JM. Stachel SJ, et al. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1122-1126. doi: 10.1016/j.bmcl.2018.01.039. Epub 2018 Feb 10. Bioorg Med Chem Lett. 2018. PMID: 29534798
Discovery of a Distinct Chemical and Mechanistic Class of Allosteric HIV-1 Integrase Inhibitors with Antiretroviral Activity.
Burlein C, Wang C, Xu M, Bhatt T, Stahlhut M, Ou Y, Adam GC, Heath J, Klein DJ, Sanders J, Narayan K, Abeywickrema P, Heo MR, Carroll SS, Grobler JA, Sharma S, Diamond TL, Converso A, Krosky DJ. Burlein C, et al. Among authors: abeywickrema p. ACS Chem Biol. 2017 Nov 17;12(11):2858-2865. doi: 10.1021/acschembio.7b00550. Epub 2017 Oct 19. ACS Chem Biol. 2017. PMID: 29024587
The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.
Sparey T, Abeywickrema P, Almond S, Brandon N, Byrne N, Campbell A, Hutson PH, Jacobson M, Jones B, Munshi S, Pascarella D, Pike A, Prasad GS, Sachs N, Sakatis M, Sardana V, Venkatraman S, Young MB. Sparey T, et al. Among authors: abeywickrema p. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3386-91. doi: 10.1016/j.bmcl.2008.04.020. Epub 2008 Apr 13. Bioorg Med Chem Lett. 2008. PMID: 18455394
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack AM, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: abeywickrema p. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3. doi: 10.1016/j.chembiol.2019.10.002. Epub 2019 Oct 22. Cell Chem Biol. 2020. PMID: 31653597 Free article.
23 results