Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2<em>H</em>)-one derivatives as novel PRMT5/MTA inhibitors

Publication date: 1 October 2022Source: Bioorganic & Medicinal Chemistry, Volume 71Author(s): Christopher R. Smith, Ruth Aranda, James G. Christensen, Lars D. Engstrom, Robin J. Gunn, Anthony Ivetac, John M. Ketcham, Jon Kuehler, J. David Lawson, Matth…

Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity

Publication date: 1 October 2022Source: Bioorganic & Medicinal Chemistry, Volume 71Author(s): Tomoyoshi Imaizumi, Michinori Akaiwa, Tomoaki Abe, Takahiro Nigawara, Takanori Koike, Yoshiki Satake, Kazushi Watanabe, Osamu Kaneko, Yasushi Amano, Kenichi M…

Corrigendum to “Synthesis and evaluation of 1,2,3-dithiazole inhibitors of the nucleocapsid protein of feline immunodeficiency virus (FIV) as a model for HIV infection” [Bioorg. Med. Chem. 68 (2022) 116834]

Publication date: Available online 29 July 2022Source: Bioorganic & Medicinal ChemistryAuthor(s): Tuomo Laitinen, Theres Meili, Maria Koyioni, Panayiotis A. Koutentis, Antti Poso, Regina Hofmann-Lehmann, Christopher R.M. Asquith

Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interaest of the salicylanilide pharmacophore in the fight against tuberculosis

Publication date: Available online 29 July 2022Source: Bioorganic & Medicinal ChemistryAuthor(s): Nguyen-Hung Le, Patricia Constant, Samuel Tranier, Virginie Nahoum, Valérie Guillet, Laurent Maveyraud, Mamadou Daffé, Lionel Mourey, Pierre Verhaeghe, He…