103264-00-2Relevant academic research and scientific papers
Palladium-Catalyzed Synthesis of Indolines from Aroyloxycarbamates through a Tandem Decarboxylative Amination/Heck/Annulation Reaction
Wang, Zheng,Li, Peihe,Fu, Hui,Dai, Qipu,Hu, Changwen
, p. 192 - 200 (2019)
A novel synthesis of functionalized indolines via a Pd-catalyzed tandem decarboxylative amination/Heck/annulation reaction has been developed. This process features operational simplicity, mild conditions, and the use of a readily available and environmentally friendly starting material, namely carboxylic acid. Furthermore, the reaction shows good functional group tolerance and chemical selectivity. (Figure presented.).
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.
Trapping reactive metal-carbene complexes by a bis-pocket porphyrin: X-ray crystal structures of Ru=CHCO2et and trans-[Ru(CHR)(CO)] species and highly selective carbenoid transfer reaction
Deng, Qing-Hai,Chen, Jian,Huang, Jie-Sheng,Chui, Stephen Sin-Yin,Zhu, Nianyong,Li, Guang-Yu,Che, Chi-Ming
experimental part, p. 10707 - 10712 (2010/04/30)
What's in my pockets? By employing Suslick's bis-pocket porphyrin (ttppp), a reactive M=CHCO2Et complex and a trans-[M(CHR)(CO)] (M = Ru) complex have been structurally characterized by X-ray crystal analysis. The sterically encumbered ttppp ligand has a significant impact on both the diastereoselectivity and chemoselectivity in metalloporphyrin-catalyzed reactions of ethyl diazoacetate with conjugated aryl dienes.
