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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: huang x. 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
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Huang C, Fischer C, Machacek MR, Bogen S, Biftu T, Huang X, Reutershan MH, Otte R, Hong Q, Wu Z, Yu Y, Park M, Chen L, Biju P, Knemeyer I, Lu P, Kochansky CJ, Hicks MB, Liu Y, Helmy R, Fradera X, Donofrio A, Close J, Maddess ML, White C, Sloman DL, Sciammetta N, Lu J, Gibeau C, Simov V, Zhang H, Fuller P, Witter D. Huang C, et al. Among authors: huang x. ACS Med Chem Lett. 2022 Mar 28;13(4):734-741. doi: 10.1021/acsmedchemlett.2c00089. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450359 Free PMC article.
SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist.
Huang X, Su J, Rao AU, Tang H, Zhou W, Zhu X, Chen X, Liu Z, Huang Y, Degrado S, Xiao D, Qin J, Aslanian R, McKittrick BA, Greenfeder S, Heek Mv, Chintala M, Palani A. Huang X, et al. Among authors: huang y. Bioorg Med Chem Lett. 2012 Jan 15;22(2):854-8. doi: 10.1016/j.bmcl.2011.12.041. Epub 2011 Dec 13. Bioorg Med Chem Lett. 2012. PMID: 22209457
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Huang X, Zhu X, Chen X, Zhou W, Xiao D, Degrado S, Aslanian R, Fossetta J, Lundell D, Tian F, Trivedi P, Palani A. Huang X, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70. doi: 10.1016/j.bmcl.2011.11.074. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22169260
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.
Qin J, Dhondi P, Huang X, Mandal M, Zhao Z, Pissarnitski D, Zhou W, Aslanian R, Zhu Z, Greenlee W, Clader J, Zhang L, Cohen-Williams M, Jones N, Hyde L, Palani A. Qin J, et al. Among authors: huang x. Bioorg Med Chem Lett. 2011 Jan 15;21(2):664-9. doi: 10.1016/j.bmcl.2010.12.012. Epub 2010 Dec 13. Bioorg Med Chem Lett. 2011. PMID: 21195610
The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.
Li H, Qin J, Dhondi P, Zhou W, Vicarel M, Bara T, Cole D, Josien H, Pissarnitski D, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Huang X. Li H, et al. Among authors: huang x. Bioorg Med Chem Lett. 2013 Jan 15;23(2):466-71. doi: 10.1016/j.bmcl.2012.11.055. Epub 2012 Nov 29. Bioorg Med Chem Lett. 2013. PMID: 23253441
Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.
Huang X, Brubaker J, Zhou W, Biju PJ, Xiao L, Shao N, Huang Y, Dong L, Liu Z, Bitar R, Buevich A, Jung J, Peterson SL, Butcher JW, Close J, Martinez M, MacCoss RN, Zhang H, Crawford S, McCormick KD, Aslanian R, Nargund R, Correll C, Gervais F, Qiu H, Yang X, Garlisi C, Rindgen D, Maloney KM, Siliphaivanh P, Palani A. Huang X, et al. Among authors: huang y. ACS Med Chem Lett. 2018 Jun 23;9(7):679-684. doi: 10.1021/acsmedchemlett.8b00145. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034600 Free PMC article.
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