Novel 3-Azaindolyl-4-arylmaleimides Exhibiting Potent Antiangiogenic Efficacy, Protein Kinase Inhibition, and Antiproliferative Activity
作者:Christopher Ganser、Eva Lauermann、Annett Maderer、Torsten Stauder、Jan-Peter Kramb、Stanislav Plutizki、Thomas Kindler、Markus Moehler、Gerd Dannhardt
DOI:10.1021/jm301217c
日期:2012.11.26
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.