4.7 Article

Novel 3-Azaindolyl-4-arylmaleimides Exhibiting Potent Antiangiogenic Efficacy, Protein Kinase Inhibition, and Antiproliferative Activity

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 22, Pages 9531-9540

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm301217c

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Funding

  1. Stiftung Rheinland-Pfalz fur Innovation

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Tumor growth and metastasis are highly associated with the overexpression of protein kinases (PKs) regulating cell growth, apoptosis resistance, and prolonged cell survival. This study describes novel azaindolyl-maleimides with significant inhibition of PKs, such as VEGFR, FLT-3, and GSK-3 beta which are related to carcinogenesis. Furthermore, these compounds exhibit high kinase selectivity and potent inhibition of angiogenesis and cell proliferation, offering versatile options in cancer treatment strategies.

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