Time filter

Source Type

Gummadi V.R.,Aurigene Discovery Technologies Ltd. and 39 40 KIADB Indus. Area Electrical City Ph II Hosur Rd. | Rajagopalan S.,Aurigene Discovery Technologies Ltd. and 39 40 KIADB Indus. Area Electrical City Ph II Hosur Rd. | Looi C.-Y.,University of Malaya | Paydar M.,University of Malaya | And 14 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

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. © 2013 Elsevier Ltd. All rights reserved.

Loading Aurigene Discovery Technologies Ltd. and 39 40 KIADB Indus. Area Electrical City Ph II Hosur Rd. collaborators
Loading Aurigene Discovery Technologies Ltd. and 39 40 KIADB Indus. Area Electrical City Ph II Hosur Rd. collaborators