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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: tang s. 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
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: tang s. 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.
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: tang s. 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: tang s. 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
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: tang s. 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: tang s. 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
Preclinical Profile of AB-423, an Inhibitor of Hepatitis B Virus Pregenomic RNA Encapsidation.
Mani N, Cole AG, Phelps JR, Ardzinski A, Cobarrubias KD, Cuconati A, Dorsey BD, Evangelista E, Fan K, Guo F, Guo H, Guo JT, Harasym TO, Kadhim S, Kultgen SG, Lee ACH, Li AHL, Long Q, Majeski SA, Mao R, McClintock KD, Reid SP, Rijnbrand R, Snead NM, Micolochick Steuer HM, Stever K, Tang S, Wang X, Zhao Q, Sofia MJ. Mani N, et al. Among authors: tang s. Antimicrob Agents Chemother. 2018 May 25;62(6):e00082-18. doi: 10.1128/AAC.00082-18. Print 2018 Jun. Antimicrob Agents Chemother. 2018. PMID: 29555628 Free PMC article.
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein.
Mani N, Cole AG, Phelps JR, Ardzinski A, Burns R, Chiu T, Cuconati A, Dorsey BD, Evangelista E, Fan K, Guo F, Harasym TO, Kadhim S, Kowalski R, Kultgen SG, Lee ACH, Li AH, Majeski SA, Miller A, Pasetka C, Reid SP, Rijnbrand R, Micolochick Steuer HM, Stever K, Tang S, Teng X, Wang X, Sofia MJ. Mani N, et al. Among authors: tang s. Antiviral Res. 2022 Jan;197:105211. doi: 10.1016/j.antiviral.2021.105211. Epub 2021 Nov 23. Antiviral Res. 2022. PMID: 34826506
Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1.
Park JJ, Thi EP, Carpio VH, Bi Y, Cole AG, Dorsey BD, Fan K, Harasym T, Iott CL, Kadhim S, Kim JH, Lee ACH, Nguyen D, Paratala BS, Qiu R, White A, Lakshminarasimhan D, Leo C, Suto RK, Rijnbrand R, Tang S, Sofia MJ, Moore CB. Park JJ, et al. Among authors: tang s. Nat Commun. 2021 Feb 22;12(1):1222. doi: 10.1038/s41467-021-21410-1. Nat Commun. 2021. PMID: 33619272 Free PMC article.
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