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Page 1
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y. Zhang H, et al. Among authors: ferguson h. ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749906 Free PMC article.
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.
Smith GF, Altman MD, Andresen B, Baker J, Brubaker JD, Chen H, Chen Y, Childers M, Donofrio A, Ferguson H, Fischer C, Fischmann TO, Gibeau C, Hicks A, Jin S, Kattar S, Kleinschek MA, Leccese E, Lesburg C, Li C, Lim J, Liu D, Maclean JKF, Mansoor F, Moy LY, Mulrooney EF, Necheva AS, Presland J, Rakhilina L, Yang R, Torres L, Zhang-Hoover J, Northrup A. Smith GF, et al. Among authors: ferguson h. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726. doi: 10.1016/j.bmcl.2017.04.050. Epub 2017 Apr 18. Bioorg Med Chem Lett. 2017. PMID: 28501511
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: ferguson h. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Pu Q, Zhang H, Guo L, Cheng M, Doty AC, Ferguson H, Fradera X, Lesburg CA, McGowan MA, Miller JR, Geda P, Song X, Otte K, Sciammetta N, Solban N, Yu W, Sloman DL, Zhou H, Lammens A, Neumann L, Bennett DJ, Pasternak A, Han Y. Pu Q, et al. Among authors: ferguson h. ACS Med Chem Lett. 2020 Jul 15;11(8):1548-1554. doi: 10.1021/acsmedchemlett.0c00195. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832022 Free PMC article.
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors.
Lacey BM, Xu Z, Chai X, Laskey J, Fradera X, Mittal P, Mishra S, Piesvaux J, Saradjian P, Shaffer L, Vassileva G, Gerdt C, Wang Y, Ferguson H, Smith DM, Ballard J, Wells S, Jain R, Mueller U, Addona G, Kariv I, Methot JL, Bittinger M, Ranganath S, Mcleod R, Pasternak A, Miller JR, Xu H. Lacey BM, et al. Among authors: ferguson h. SLAS Discov. 2021 Jan;26(1):88-99. doi: 10.1177/2472555220952071. Epub 2020 Aug 26. SLAS Discov. 2021. PMID: 32844715 Free article.
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: ferguson h. 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: ferguson h. 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
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.
Yu W, Deng Y, Sloman D, Li D, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Richard Miller J, Knemeyer I, Otte K, Vincent S, Sciammetta N, Jonathan Bennett D, Han Y. Yu W, et al. Among authors: ferguson h. Bioorg Med Chem Lett. 2021 Oct 1;49:128314. doi: 10.1016/j.bmcl.2021.128314. Epub 2021 Aug 13. Bioorg Med Chem Lett. 2021. PMID: 34391891
STimulator of INterferon Genes Agonism Accelerates Antitumor Activity in Poorly Immunogenic Tumors.
Perera SA, Kopinja JE, Ma Y, Muise ES, Laskey J, Chakravarthy K, Chen Y, Cui L, Presland J, Sathe M, Javaid S, Minnihan EC, Ferguson HM, Piesvaux J, Pan BS, Zhao S, Sharma SK, Woo HC, Pucci V, Knemeyer I, Cemerski S, Cumming J, Trotter BW, Tse A, Khilnani A, Ranganath S, Long BJ, Bennett DJ, Addona GH. Perera SA, et al. Among authors: ferguson hm. Mol Cancer Ther. 2022 Feb;21(2):282-293. doi: 10.1158/1535-7163.MCT-21-0136. Epub 2021 Nov 23. Mol Cancer Ther. 2022. PMID: 34815361
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.
Li D, Sloman DL, Achab A, Zhou H, McGowan MA, White C, Gibeau C, Zhang H, Pu Q, Bharathan I, Hopkins B, Liu K, Ferguson H, Fradera X, Lesburg CA, Martinot TA, Qi J, Song ZJ, Yin J, Zhang H, Song L, Wan B, DAddio S, Solban N, Miller JR, Zamlynny B, Bass A, Freeland E, Ykoruk B, Hilliard C, Ferraro J, Zhai J, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: ferguson h. J Med Chem. 2022 Apr 28;65(8):6001-6016. doi: 10.1021/acs.jmedchem.1c01670. Epub 2022 Mar 3. J Med Chem. 2022. PMID: 35239336
567 results