Document Type
Article (Restricted)
Publication Date
1-1-2013
Abstract
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 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. (C) 2013 Elsevier Ltd. All rights reserved.
Keywords
Anaplastic lymphoma kinase (ALK), 7-Azaindole, Anaplastic large cell lymphoma (ALCL), Cancer, Karpas299
Divisions
fac_med
Publication Title
Bioorganic & Medicinal Chemistry Letters
Volume
23
Issue
17
Additional Information
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