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Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.
Crosignani S, Bingham P, Bottemanne P, Cannelle H, Cauwenberghs S, Cordonnier M, Dalvie D, Deroose F, Feng JL, Gomes B, Greasley S, Kaiser SE, Kraus M, Négrerie M, Maegley K, Miller N, Murray BW, Schneider M, Soloweij J, Stewart AE, Tumang J, Torti VR, Van Den Eynde B, Wythes M. Crosignani S, et al. Among authors: gomes b. J Med Chem. 2017 Dec 14;60(23):9617-9629. doi: 10.1021/acs.jmedchem.7b00974. Epub 2017 Nov 21. J Med Chem. 2017. PMID: 29111717
Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.
Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M. Gomes B, et al. Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19. Mol Cancer Ther. 2018. PMID: 30232146
Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenylpyridin-2-one trifluoromethyl ketones.
Bernstein PR, Andisik D, Bradley PK, Bryant CB, Ceccarelli C, Damewood JR Jr, Earley R, Edwards PD, Feeney S, Gomes BC, et al. Bernstein PR, et al. Among authors: gomes bc. J Med Chem. 1994 Sep 30;37(20):3313-26. doi: 10.1021/jm00046a016. J Med Chem. 1994. PMID: 7932559
Anticancer activity of koningic acid and semisynthetic derivatives.
Rahier NJ, Molinier N, Long C, Deshmukh SK, Kate AS, Ranadive P, Verekar SA, Jiotode M, Lavhale RR, Tokdar P, Balakrishnan A, Meignan S, Robichon C, Gomes B, Aussagues Y, Samson A, Sautel F, Bailly C. Rahier NJ, et al. Among authors: gomes b. Bioorg Med Chem. 2015 Jul 1;23(13):3712-21. doi: 10.1016/j.bmc.2015.04.004. Epub 2015 Apr 9. Bioorg Med Chem. 2015. PMID: 25937235
Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.
Edwards PD, Andisik DW, Bryant CA, Ewing B, Gomes B, Lewis JJ, Rakiewicz D, Steelman G, Strimpler A, Trainor DA, Tuthill PA, Mauger RC, Veale CA, Wildonger RA, Williams JC, Wolanin DJ, Zottola M. Edwards PD, et al. Among authors: gomes b. J Med Chem. 1997 Jun 6;40(12):1876-85. doi: 10.1021/jm960819g. J Med Chem. 1997. PMID: 9191965
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