214485-69-5Relevant articles and documents
Quinoline and quinazoline derivatives, preparation method, intermediate, composition and use thereof (by machine translation)
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, (2016/11/07)
The invention discloses a quinoline and quinazoline derivative I, a preparation method, an intermediate C, composition and an application. The preparation method comprises two methods, wherein the first method comprises steps as follows: 1, a compound A and a compound B react in a solvent under the action of alkali 1 to obtain a compound C; and 2, the product C obtained in the step 1 reacts with a compound D under the action of alkali 2; and the second comprises step as follows: the compound A and a compound E react in the solvent under the action of the alkali 1. The invention further provides the application of the compound represented in formula I or medicine composition in preparation of an EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor, an A431 or H1975 cell proliferation inhibitor or medicine for preventing or treating tumor diseases. The provided compound has better antitumor activity.
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epi
Wissner, Allan,Overbeek, Elsebe,Reich, Marvin F.,Floyd, M. Brawner,Johnson, Bernard D.,Mamuya, Nellie,Rosfjord, Edward C.,Discafani, Carolyn,Davis, Rachel,Shi, Xiaoqing,Rabindran, Sridhar K.,Gruber, Brian C.,Ye, Fei,Hallett, William A.,Nilakantan, Ramaswamy,Shen, Ru,Wang, Yu-Fen,Greenberger, Lee M.,Tsou, Hwei-Ru
, p. 49 - 63 (2007/10/03)
A series of of 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile derivatives that function as irreversible inhibitors of EGFR and HER-2 kinases have been prepared. These inhibitors have, at the 6-position, butynamide, crotonamide, and methacrylamide Mic