80171-41-1Relevant academic research and scientific papers
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.
Substituents Effect on the Reaction of Aromatic Acetals Over Aluminium Phosphate and Aluminium Sulphate Catalyst
Xavier, N.,Arulraj, S. J.
, p. 775 - 777 (2007/10/02)
Aromatic acetals in the presence of aluminium phosphate (AP) catalyst at elevated temperatures yield the corresponding esters (b), ethers (c) and the parent aldehydes (d).These substrates over aluminium sulphate (AS) catalyst give only the esters (b) and aldehydes (d).The products distribution varies with temperature.Substituents in the ring also play a part in the reaction.
REARRANGEMENT OF SUBSTITUTED AROMATIC ACETALS CATALYSED BY γ-ALUMINA
Xavier, N.,Arulraj, S. J.
, p. 2875 - 2878 (2007/10/02)
Aromatic acetals over γ-alumina undergo rearrangement to give the corresponding esters (b) and ethers (c) in good yield.The product distribution varied unusually over the range of reaction temperatures.The effect of substituents has also been felt much in the study.Probable mechanisms have been suggested for the reaction.The catalyst has been characterized by various studies and the specific poisoning of the catalyst has been done with NH3, CO2 and H2S.
