Discovery of a new class of potent pyrrolo[3,4-c]quinoline-1,3-diones based inhibitors of human dihydroorotate dehydrogenase: Synthesis, pharmacological and toxicological evaluation

• Published in: Bioorganic chemistry Vol. 147; p. 107359
• Main Authors: Dimitrijević, Marina G., Roschger, Cornelia, Lang, Kevin, Zierer, Andreas, Paunović, Milica G., Obradović, Ana D., Matić, Miloš M., Pocrnić, Marijana, Galić, Nives, Ćirić, Andrija, Joksović, Milan D.
• Format: Journal Article
• Language: English
• Published: SAN DIEGO Elsevier Inc 01.06.2024; Elsevier
• Subjects: Biochemistry & Molecular Biology; Chemistry; Chemistry, Organic; Dihydroorotate dehydrogenase; hDHODH inhibitors; Life Sciences & Biomedicine; Lipophilicity; Physical Sciences; Pyrrolo[3,4-c]quinolones; Science & Technology; Toxicology; hDHODH inhibitors; Toxicology; Pyrrolo[3,4-c]quinolones; Dihydroorotate dehydrogenase; Lipophilicity; SURVIVAL; GAMMA; Pyrrolo; CELLS; ASSAY; HEPATOTOXICITY; c ]quinolones; LEFLUNOMIDE

[Display omitted] •Pyrrolo[3,4-c]quinoline-1,3-diones were prepared by cyclization cascade reactions.•New class of potent hDHODH inhibitory demonstrated better activity than leflunomide.•Very low cytotoxicity against healthy HaCaT cells was observed.•The optimal lipophilicity was determined at physi...