40232-88-0Relevant articles and documents
Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant
Fukuda, Tsutomu,Umeki, Teppei,Tokushima, Keiji,Xiang, Gao,Yoshida, Yuki,Ishibashi, Fumito,Oku, Yusuke,Nishiya, Naoyuki,Uehara, Yoshimasa,Iwao, Masatomo
, p. 6563 - 6580 (2017/11/17)
A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile against the T790M/L858R mutant [IC50 (WT) = 31.8 nM; IC50 (T790M/L858R) = 8.9 nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.
New approach for the construction of the coumarin frame and application in the total synthesis of natural products
Jerezano, Alberto,Jimenez, Fabiola,Del Carmen Cruz, Maria,Montiel, Luisa E.,Delgado, Francisco,Tamariz, Joaquin
experimental part, p. 185 - 198 (2011/04/17)
A new synthetic approach is described for building the coumarin scaffold through the Lewis acid-promoted cyclization of novel aryl 3-(dimethylamino)prop- 2-enoates 2a - 2f. The latter precursors were prepared via aminomethylenation of the corresponding aryl acetates 4a - 4f with the Bredereck reagent. This approach was used for the synthesis of biologically active natural compounds 1a - 1f, through a three-step procedure starting from the corresponding phenols.
Improved solvent-free Dakin oxidation protocol
Da Silva, Emerson Teixeira,Camara, Celso Amorim,Antunes,Barreiro, Eliezer J.,Fraga, Carlos A. M.
, p. 784 - 788 (2008/09/16)
A solvent-free Dakin reaction with mCPBA was accomplished with various aromatic aldehydes, resulting in an easy and improved methodology for the preparation of corresponding phenols. 3,4-Methylenedioxyphenol, 3,4-dimethoxyphenol, 4-methoxyphenol, 4-chlorophenol, and other functionalized phenols were obtained in high yields from the corresponding aromatic aldehydes in a few minutes. This new methodology represents an efficient alternative for this important synthetic conversion. Copyright Taylor & Francis Group, LLC.
