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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: graves ie. 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
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: graves ie. 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. 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
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: graves ie. 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: graves ie. Antiviral Res. 2024 Nov;231:106010. doi: 10.1016/j.antiviral.2024.106010. Epub 2024 Sep 24. Antiviral Res. 2024. PMID: 39326502