7115-91-5Relevant articles and documents
Metal Complexes with Macrocyclic Ligands Part XXV One-Step Synthesis of Mono-N-substituted Azamacrocycles with a Carboxylic Group in the Side-Chain and their Complexes with Cu2+ and Ni2+
Studer, Martin,Kaden, Thomas A.
, p. 2081 - 2086 (1986)
Mono-N-substituted azamacrocycles 2-7, containing a carboxyalkyl or carboxyaryl side-chain, are obtained by reacting a five-fold excess of the macrocycle with 1 equiv. of a suitable halogenocarboxylic acid in alkaline aqueous EtOH.For halogenocarboxylic a
Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid
Mélin, Léa,Abdullayev, Shuay,Fnaiche, Ahmed,Vu, Victoria,González Suárez, Narjara,Zeng, Hong,Szewczyk, Magdalena M.,Li, Fengling,Senisterra, Guillermo,Allali-Hassani, Abdellah,Chau, Irene,Dong, Aiping,Woo, Simon,Annabi, Borhane,Halabelian, Levon,LaPlante, Steven R.,Vedadi, Masoud,Barsyte-Lovejoy, Dalia,Santhakumar, Vijayaratnam,Gagnon, Alexandre
, p. 2982 - 3002 (2021/08/03)
The YAP-TEAD transcriptional complex is responsible for the expression of genes that regulate cancer cell growth and proliferation. Dysregulation of the Hippo pathway due to overexpression of TEAD has been reported in a wide range of cancers. Inhibition of TEAD represses the expression of associated genes, demonstrating the value of this transcription factor for the development of novel anti-cancer therapies. We report herein the design, synthesis and biological evaluation of LM98, a flufenamic acid analogue. LM98 shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity. Binding of LM98 to TEAD was supported by 19F-NMR studies while co-crystallization experiments confirmed that LM98 is anchored within the palmitic acid pocket of TEAD. LM98 reduces the expression of CTGF and Cyr61, inhibits MDA-MB-231 breast cancer cell migration and arrests cell cycling in the S phase during cell division.
Influenza virus replication inhibitor and uses thereof
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, (2020/05/05)
The invention belongs to the field of medicines, and particularly relates to a new compound serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition in the treatment of influenza. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the compound shown in the formula (I). The compound can well inhibit influenza viruses, and/or has lowercytotoxicity, more excellent in-vivo metabolic dynamics properties and in-vivo pharmacodynamic properties.