1616628-98-8Relevant articles and documents
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors
Daydé-Cazals, Bénédicte,Fauvel, Bénédicte,Singer, Mathilde,Feneyrolles, Clémence,Bestgen, Benoit,Gassiot, Fanny,Spenlinhauer, Aurélia,Warnault, Pierre,Van Hijfte, Nathalie,Borjini, Nozha,Chevé, Gwéna?l,Yasri, Abdelaziz
, p. 3886 - 3905 (2016/05/24)
Efforts were made to improve a series of potent dual ABL/SRC inhibitors based on a 7-azaindole core with the aim of developing compounds that demonstrate a wider activity on selected oncogenic kinases. Multi-targeted kinase inhibitors (MTKIs) were then derived, focusing on kinases involved in both angiogenesis and tumorigenesis processes. Antiproliferative activity studies using different cellular models led to the discovery of a lead candidate (6z) that combined both antiangiogenic and antitumoral effects. The activity of 6z was assessed against a panel of kinases and cell lines including solid cancers and leukemia cell models to explore its potential therapeutic applications. With its potency and selectivity for oncogenic kinases, 6z was revealed to be a focused MTKI that should have a bright future in fighting a wide range of cancers.
AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES
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Page/Page column 40-41, (2014/07/21)
The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus a
