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Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D. Rew Y, et al. Among authors: du x. J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23. J Med Chem. 2018. PMID: 30091920
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
Du X, Moore J, Blank BR, Eksterowicz J, Sutimantanapi D, Yuen N, Metzger T, Chan B, Huang T, Chen X, Chen Y, Duong F, Kong W, Chang JH, Sun J, Zavorotinskaya T, Ye Q, Junttila MR, Ndubaku C, Friedman LS, Fantin VR, Sun D. Du X, et al. J Med Chem. 2020 Sep 24;63(18):10433-10459. doi: 10.1021/acs.jmedchem.0c01086. Epub 2020 Sep 9. J Med Chem. 2020. PMID: 32865411
Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
Du X, Chen X, Mihalic JT, Deignan J, Duquette J, Li AR, Lemon B, Ma J, Miao S, Ebsworth K, Sullivan TJ, Tonn G, Collins TL, Medina JC. Du X, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):608-13. doi: 10.1016/j.bmcl.2007.11.072. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18063364
Discovery of potent and specific CXCR3 antagonists.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Chen X, et al. Among authors: du x. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22130135
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC. Wang Y, et al. Among authors: du x. ACS Med Chem Lett. 2013 May 7;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900707 Free PMC article.
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC. Li AR, et al. Among authors: du x. Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061451
Imidazo-pyrazine derivatives as potent CXCR3 antagonists.
Du X, Gustin DJ, Chen X, Duquette J, McGee LR, Wang Z, Ebsworth K, Henne K, Lemon B, Ma J, Miao S, Sabalan E, Sullivan TJ, Tonn G, Collins TL, Medina JC. Du X, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5200-4. doi: 10.1016/j.bmcl.2009.07.021. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19631529
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