110523-76-7Relevant academic research and scientific papers
Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold
Kawai, Junya,Ota, Masahiro,Ohki, Hitoshi,Toki, Tadashi,Suzuki, Makoto,Shimada, Takashi,Matsui, Satoshi,Inoue, Hidekazu,Sugihara, Chika,Matsuhashi, Norikazu,Matsui, Yumi,Takaishi, Sachiko,Nakayama, Kiyoshi
supporting information, p. 893 - 898 (2019/06/07)
Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) plays a key role in one-carbon (1C) metabolism in human mitochondria, and its high expression correlates with poor survival of patients with various types of cancer. An isozyme-selective MTHFD2 inhibitor is highly attractive for potential use in cancer treatment. Herein, we disclose a novel isozyme-selective MTHFD2 inhibitor DS44960156, with a tricyclic coumarin scaffold, which was initially discovered via high-throughput screening (HTS) and improved using structure-based drug design (SBDD). DS44960156 would offer a good starting point for further optimization based on the following features: (1) unprecedented selectivity (>18-fold) for MTHFD2 over MTHFD1, (2) a molecular weight of less than 400, and (3) good ligand efficiency (LE).
A New Route to 6-Azachromones. An Improved Synthesis of 2-Azaxanthone
Cordonnier, Guy,Sliwa, Henri
, p. 111 - 115 (2007/10/02)
Condensation of the morpholine enamine of 1-benzyl-4-piperidone with β-ketoesters yielded 6-azatetrahydrochromones which were debenzylated and aromatized to 6-azachromones; 2-azaxanthone has been thus obtained with an improved yield as compared to previous syntheses.
