1240322-48-8Relevant academic research and scientific papers
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.
DERIVATIVES OF AZAINDOLES AS INHIBITORS OF PROTEIN KINASES ABL AND SRC
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Page/Page column 96; 98-99, (2010/09/03)
The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medicinal products comprising these compounds.
