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Studies on 5-Substituted N-Aryl or 3-Aryl-Indole Derivatives as Potential RTK Inhibitors

초록/요약

Receptor Tyrosine Kinase (RTK) has been known as the promising target for an anticancer drug. Recently, several RTK inhibitors launched as anti-cancer drugs and showed good profiles clinically, but it still needs to find novel RTK inhibitors, especially to overcome the resistance. We identified the 5-substituted indoles as RTK inhibitors, and investigated the influence of various 5-substituents on the activity, including aryl rings, amines, amides, or ureas, and etc. Using 5-nitro indoles, we synthesized 3-aryl or N-aryl derivatives with 5-substiuents, and evaluated their inhibitory activities on VEGF-, or EGF-RTK. Also, the inhibitory effects on human tumor cell growth were examined.

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