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Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin-3 Inhibitors.
Xu L, Hartz RA, Beno BR, Ghosh K, Shukla JK, Kumar A, Patel D, Kalidindi N, Lemos N, Gautam SS, Kumar A, Ellsworth BA, Shah D, Sale H, Cheng D, Regueiro-Ren A. Xu L, et al. Among authors: cheng d. J Med Chem. 2021 May 27;64(10):6634-6655. doi: 10.1021/acs.jmedchem.0c02001. Epub 2021 May 14. J Med Chem. 2021. PMID: 33988358
Identification of Monosaccharide Derivatives as Potent, Selective, and Orally Bioavailable Inhibitors of Human and Mouse Galectin-3.
Liu C, Jalagam PR, Feng J, Wang W, Raja T, Sura MR, Manepalli RKVLP, Aliphedi BR, Medavarapu S, Nair SK, Muthalagu V, Natesan R, Gupta A, Beno B, Panda M, Ghosh K, Shukla JK, Sale H, Haldar P, Kalidindi N, Shah D, Patel D, Mathur A, Ellsworth BA, Cheng D, Regueiro-Ren A. Liu C, et al. Among authors: cheng d. J Med Chem. 2022 Aug 25;65(16):11084-11099. doi: 10.1021/acs.jmedchem.2c00517. Epub 2022 Aug 15. J Med Chem. 2022. PMID: 35969688
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Moore F, Wang W, Zhao G, Mignone J, Meng W, Chu CH, Ma Z, Azzara A, Cullen MJ, Pelleymounter MA, Appiah K, Cvijic ME, Dierks E, Chang S, Foster K, Kopcho L, O'Malley K, Li YX, Khandelwal P, Whaley JM, Mathur A, Hou X, Wu DR, Robl JA, Cheng D, Devasthale P. Moore F, et al. Among authors: cheng d. Bioorg Med Chem Lett. 2023 Jul 15;91:129362. doi: 10.1016/j.bmcl.2023.129362. Epub 2023 Jun 8. Bioorg Med Chem Lett. 2023. PMID: 37295614
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design.
Liu C, Wang W, Feng J, Beno B, Raja T, Swidorski J, Manepalli RKVLP, Vetrichelvan M, Rao Jalagam P, Nair SK, Gupta A, Panda M, Ghosh K, Kaushikkumar Shukla J, Sale H, Shah D, Singh Gautam S, Patel D, Mathur A, Ellsworth BA, Cheng D, Regueiro-Ren A. Liu C, et al. Among authors: cheng d. Bioorg Med Chem. 2024 Mar 1;101:117638. doi: 10.1016/j.bmc.2024.117638. Epub 2024 Feb 11. Bioorg Med Chem. 2024. PMID: 38394996
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione.
Yoon DS, Liu C, Jalagam PR, Feng J, Wang W, Swidorski JJ, Xu L, Hartz RA, Nair SK, Beno BR, Panda M, Ghosh K, Kumar A, Sale H, Shah D, Mathur A, Ellsworth BA, Cheng D, Regueiro-Ren A. Yoon DS, et al. Among authors: cheng d. J Med Chem. 2024 Aug 22;67(16):14184-14199. doi: 10.1021/acs.jmedchem.4c01008. Epub 2024 Aug 5. J Med Chem. 2024. PMID: 39102502
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P. Turdi H, et al. Among authors: cheng d. J Med Chem. 2021 Oct 14;64(19):14773-14792. doi: 10.1021/acs.jmedchem.1c01356. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34613725
4,799 results