133303-87-4Relevant academic research and scientific papers
Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
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, (2008/06/13)
Disclosed are pyrrolopyridazine compounds, methods of preparing such compounds, and their use for the treatment of proliferative, inflammatory, and other disorders.
Synthesis and evaluation of 4-anilino-6, 7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade
Berger, Dan,Dutia, Minu,Powell, Dennis,Wu, Biqi,Wissner, Allan,Boschelli, Diane H.,Floyd, M. Brawner,Zhang, Nan,Torres, Nancy,Levin, Jeremy,Du, Xuemei,Wojciechowicz, Donald,Discafani, Carolyn,Kohler, Constance,Kim, Steven C.,Feldberg, Larry R.,Collins, Karen,Mallon, Robert
, p. 3031 - 3034 (2007/10/03)
4-[3-Chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)]anilino-6, 7-diethoxy-3-quinolinecarbonitrile (3) was identified as a MEK1 kinase inhibitor with exceptional activity against LoVo cells. The structure-activity relationships of the C-4 aniline substituents were explored, and water-solubilizing groups were added at the C-7 position to improve physical properties. Secondary cellular assays revealed that a compound possessing the appropriate aniline substituents inhibited MEK1 as well as MAPK phosphorylation, thereby acting as a dual inhibitor of the Ras-MAPK signaling cascade.
Aniline derivatives
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, (2008/06/13)
The invention concerns aniline derivatives of formula I STR1 wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3 heteroatoms selected from oxygen, nitrogen and sulfur, and X, R1 and R2 are defined in the claims; or pharmaceutical compositions containing them, and the methods of using the compounds as tyrosine kinase inhibitors and for the treatment of proliferative diseases such as cancer.
