Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: Wild type and mutant (L1196M) active compounds with unique binding mode

• Main Authors: Gummadi, V.R., Rajagopalan, S., Looi, C.Y., Paydar, M., Renukappa, G.A., Ainan, B.R., Krishnamurthy, N.R., Panigrahi, S.K., Mahasweta, K., Raghuramachandran, S., Rajappa, M., Ramanathan, A., Lakshminarasimhan, A., Ramachandra, M., Wong, Pooi Fong, Mustafa, Mohd Rais, Nanduri, S., Hosahalli, S.
• Format: Article
• Language: English
• Published: 2013
• Subjects: R Medicine
• Online Access: http://eprints.um.edu.my/8532/1/Gummadi-2013-Discovery_of_7-azain.pdf; http://eprints.um.edu.my/8532/; http://www.sciencedirect.com/science/article/pii/S0960894X13008044

We have identified a novel 7-azaindole series of anaplastic lymphoma kinase (ALK) inhibitors. Compounds 7h, 7m and 7n demonstrate excellent potencies in biochemical and cellular assays. X-ray crystal structure of one of the compounds (7k) revealed a unique binding mode with the benzyl group occupyin...