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Page 1
Structure-Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2',1':2,3]imidazo[4,5-h]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer.
Gotchev D, Chen S, Dugan B, Dorsey BD, Wang X, Sheraz M, Kowalski R, Liu F, Tang S, Chiu T, Harasym T, Graves IE, Thi EP, Mason JD, Overholt N, Dugyala R, Lam AM, Cole AG, Sofia MJ. Gotchev D, et al. Among authors: harasym t. J Med Chem. 2024 Nov 28;67(22):20467-20494. doi: 10.1021/acs.jmedchem.4c01928. Epub 2024 Nov 8. J Med Chem. 2024. PMID: 39513566
Design, synthesis, and structure-activity relationship of a bicyclic HBV capsid assembly modulator chemotype leading to the identification of clinical candidate AB-506.
Cole AG, Kultgen SG, Mani N, Quintero JG, Yi Fan K, Ardzinski A, Stever K, Dorsey BD, Phelps JR, Lee ACH, Thi EP, Chiu T, Tang S, Horanyi PS, Mayclin SJ, Harasym TO, Sofia MJ. Cole AG, et al. Among authors: harasym to. Bioorg Med Chem Lett. 2023 Oct 1;94:129456. doi: 10.1016/j.bmcl.2023.129456. Epub 2023 Aug 25. Bioorg Med Chem Lett. 2023. PMID: 37633618
Structure-Activity Relationships and Discovery of (S)-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6H-pyrido[1,2-h][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer.
Gotchev D, Dorsey BD, Nguyen D, Kakarla R, Dugan B, Chen S, Gao M, Bailey L, Liu F, Harasym T, Chiu T, Tang S, Lee AC, Cole AG, Sofia MJ. Gotchev D, et al. Among authors: harasym t. J Med Chem. 2024 Jan 25;67(2):1421-1446. doi: 10.1021/acs.jmedchem.3c01981. Epub 2024 Jan 8. J Med Chem. 2024. PMID: 38190324
Preclinical Antiviral and Safety Profiling of the HBV RNA Destabilizer AB-161.
Lam AM, Dugyala RR, Sheraz M, Liu F, Thi EP, Graves IE, Cuconati A, Steuer HM, Ardzinski A, Overholt N, Mason JD, Gotchev D, Cole AG, Harasym TO, Sofia MJ. Lam AM, et al. Among authors: harasym to. Viruses. 2024 Feb 21;16(3):323. doi: 10.3390/v16030323. Viruses. 2024. PMID: 38543689 Free PMC article.
Rational Design, Synthesis, and Structure-Activity Relationship of a Novel Isoquinolinone-Based Series of HBV Capsid Assembly Modulators Leading to the Identification of Clinical Candidate AB-836.
Cole AG, Kultgen SG, Mani N, Fan KY, Ardzinski A, Stever K, Dorsey BD, Mesaros EF, Thi EP, Graves I, Tang S, Harasym TO, Lee ACH, Olland A, Suto RK, Sofia MJ. Cole AG, et al. Among authors: harasym to. J Med Chem. 2024 Sep 26;67(18):16773-16795. doi: 10.1021/acs.jmedchem.4c01568. Epub 2024 Sep 4. J Med Chem. 2024. PMID: 39231272
Conformationally Constrained Isoquinolinones as Orally Efficacious Hepatitis B Capsid Assembly Modulators.
Mesaros EF, Cole AG, Kultgen SG, Mani N, Fan KY, Dugan BJ, Ardzinski A, Stever K, Micolochick Steuer HM, Graves I, Tang S, Harasym TO, Lam AM, Thi EP, Dorsey BD, Sofia MJ. Mesaros EF, et al. Among authors: harasym to. ACS Med Chem Lett. 2024 Sep 3;15(9):1627-1634. doi: 10.1021/acsmedchemlett.4c00388. eCollection 2024 Sep 12. ACS Med Chem Lett. 2024. PMID: 39291037
Discovery of C-Linked Nucleoside Analogues with Antiviral Activity against SARS-CoV-2.
Mesaros EF, Dugan BJ, Gao M, Sheraz M, McGovern-Gooch K, Xu F, Fan KY, Nguyen D, Kultgen SG, Lindstrom A, Stever K, Tercero B, Binder RJ, Liu F, Micolochick Steuer HM, Mani N, Harasym TO, Thi EP, Cuconati A, Dorsey BD, Cole AG, Lam AM, Sofia MJ. Mesaros EF, et al. Among authors: harasym to. ACS Infect Dis. 2024 May 10;10(5):1780-1792. doi: 10.1021/acsinfecdis.4c00122. Epub 2024 Apr 23. ACS Infect Dis. 2024. PMID: 38651692
Control of Hepatitis B Virus with Imdusiran, a Small Interfering RNA Therapeutic.
Thi EP, Ye X, Snead NM, Lee ACH, Micolochick Steuer HM, Ardzinski A, Graves IE, Espiritu C, Cuconati A, Abbott C, Jarosz A, Teng X, Paratala B, McClintock K, Harasym T, Rijnbrand R, Lam AM, Sofia MJ. Thi EP, et al. Among authors: harasym t. ACS Infect Dis. 2024 Oct 11;10(10):3640-3649. doi: 10.1021/acsinfecdis.4c00514. Epub 2024 Sep 22. ACS Infect Dis. 2024. PMID: 39306863
Preclinical and clinical antiviral characterization of AB-836, a potent capsid assembly modulator against hepatitis B virus.
Lam AM, Mani N, Ardzinski A, Stever K, Cuconati A, Micolochick Steuer H, Thi EP, Graves IE, Espiritu CL, Mesaros E, Kultgen SG, Fan K, Cole AG, Harasym TO, Rijnbrand R, Brown J, Eley T, Varughese T, Gane E, Picchio G, Sims KD, Sofia MJ. Lam AM, et al. Among authors: harasym to. Antiviral Res. 2024 Nov;231:106010. doi: 10.1016/j.antiviral.2024.106010. Epub 2024 Sep 24. Antiviral Res. 2024. PMID: 39326502
The identification of highly efficacious functionalised tetrahydrocyclopenta[c]pyrroles as inhibitors of HBV viral replication through modulation of HBV capsid assembly.
Cole AG, Kultgen SG, Mani N, Ardzinski A, Fan KY, Thi EP, Dorsey BD, Stever K, Chiu T, Tang S, Daly O, Phelps JR, Harasym T, Olland A, Suto RK, Sofia MJ. Cole AG, et al. Among authors: harasym t. RSC Med Chem. 2022 Jan 19;13(3):343-349. doi: 10.1039/d1md00318f. eCollection 2022 Mar 23. RSC Med Chem. 2022. PMID: 35434625 Free PMC article.
39 results