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

作者：Ganser Christopher; Lauermann Eva; Maderer Annett; Stauder Torsten; Kramb Jan Peter; Plutizki Stanislav; Kindler Thomas; Moehler Markus; Dannhardt Gerd^*

来源：Journal of Medicinal Chemistry, 2012, 55(22): 9531-9540.

DOI：10.1021/jm301217c

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.

• 出版日期2012-11-22