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Publikationer i urvalet

9 träffar

Bibliografisk träff 2022-03-08

Discovery of tricyclic HIV-1 integrase-LEDGF/p75 allosteric inhibitors by intramolecular direct arylation reaction.

Taoda Y, Akiyama T, Tomita K, Fujiwara-Kitamura M, Tamura Y, Kawasuji T, Matsuoka E, Akihisa E, Seki T, Yoshinaga T.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2022.128664

Bibliografisk träff 2022-03-02

Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs.

Naidu BN, Patel M, McAuliffe B, Ding B, Cianci C, Simmermacher J, Jenkins S, Parker DD, Sivaprakasam P, Khan JA, Kish K, Lewis H, Hanumegowda U, Krystal M, Meanwell NA, Kadow JF.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.1c02169

Bibliografisk träff 2020-12-11

Discovery of novel HIV-1 integrase-LEDGF/p75 allosteric inhibitors based on a pyridine scaffold forming an intramolecular hydrogen bond.

Sugiyama S, Akiyama T, Taoda Y, Iwaki T, Matsuoka E, Akihisa E, Seki T, Yoshinaga T, Kawasuji T.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2020.127742

Bibliografisk träff 2020-07-10

Discovery of novel integrase-LEDGF/p75 allosteric inhibitors based on a benzene scaffold.

Sugiyama S, Iwaki T, Tamura Y, Tomita K, Matsuoka E, Arita S, Seki T, Yoshinaga T, Kawasuji T.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2020.115643

Bibliografisk träff 2020-02-21

Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.

Li G, Meanwell NA, Krystal MR, Langley DR, Naidu BN, Sivaprakasam P, Lewis H, Kish K, Khan JA, Ng A, Trainor GL, Cianci C, Dicker IB, Walker MA, Lin Z, Protack T, Discotto L, Jenkins S, Gerritz SW, Pendri A.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.9b01681

Bibliografisk träff 2019-01-18

5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site Inhibitors.

Peese KM, Allard CW, Connolly T, Johnson BL, Li C, Patel M, Sorensen ME, Walker MA, Meanwell NA, McAuliffe B, Minassian B, Krystal M, Parker DD, Lewis HA, Kish K, Zhang P, Nolte RT, Simmermacher J, Jenkins S, Cianci C, Naidu BN.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01473

Bibliografisk träff 2016-06-09

Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.

Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00194

Bibliografisk träff 2014-04-16

Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.

Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500110j

Bibliografisk träff 2014-01-22

Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.

Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500002n