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  • Title: Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: wild type and mutant (L1196M) active compounds with unique binding mode.
    Author: Gummadi VR, Rajagopalan S, Looi CY, Paydar M, Renukappa GA, Ainan BR, Krishnamurthy NR, Panigrahi SK, Mahasweta K, Raghuramachandran S, Rajappa M, Ramanathan A, Lakshminarasimhan A, Ramachandra M, Wong PF, Mustafa MR, Nanduri S, Hosahalli S.
    Journal: Bioorg Med Chem Lett; 2013 Sep 01; 23(17):4911-8. PubMed ID: 23880539.
    Abstract:
    We have identified a novel 7-azaindole series of anaplastic lymphoma kinase (ALK) inhibitors. Compounds 7b, 7 m and 7 n demonstrate excellent potencies in biochemical and cellular assays. X-ray crystal structure of one of the compounds (7 k) 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.
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