1450642-59-7Relevant articles and documents
Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: Wild type and mutant (L1196M) active compounds with unique binding mode
Gummadi, Venkateshwar Rao,Rajagopalan, Sujatha,Looi, Chung-Yeng,Paydar, Mohammadjavad,Renukappa, Girish Aggunda,Ainan, Bharathi Raja,Krishnamurthy, Narasimha Rao,Panigrahi, Sunil Kumar,Mahasweta, Kumari,Raghuramachandran, Sangeetha,Rajappa, Manoj,Ramanathan, Anuradha,Lakshminarasimhan, Anirudha,Ramachandra, Murali,Wong, Pooi-Fong,Mustafa, Mohammad Rais,Nanduri, Srinivas,Hosahalli, Subramanya
, p. 4911 - 4918 (2013/09/02)
We have identified a novel 7-azaindole series of anaplastic lymphoma kinase (ALK) inhibitors. Compounds 7b, 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 occupying the back pocket, explaining its potency towards ALK and selectivity over tested kinases particularly Aurora-A. This binding mode is in contrast to that of known ALK inhibitors such as Crizotinib and NVP-TAE684 which occupy the ribose binding pocket, close to DFG motif.