Lee, Soyoung published the artcileDevelopment and Biological Evaluation of Potent and Selective c-KITD816V Inhibitors, Quality Control of 757978-19-1, the publication is Journal of Medicinal Chemistry (2014), 57(15), 6428-6443, database is CAplus and MEDLINE.
The c-KIT tyrosine kinase has emerged as a potential therapeutic target for an array of diseases. However, there exists a drug resistance that is caused by mutations in c-KIT; therefore, c-KIT remains as a clin. challenge due to limited effective treatment options for therapies. For example, the acquired activating point mutation D816V significantly impairs the efficacy of targeted cancer therapies. Understanding the mechanisms of drug resistance at the mol. level will aid in designing and developing particular inhibitors with the potential to overcome these resistance mutations. The authors undertake a structure-based de novo design of 7-azaindole as the mol. core using the modified scoring function. This approach led to an identification of new c-KIT inhibitors over 100-fold specific for the D816V mutant relative to the wild-type c-KIT with nanomolar inhibitory activity. More importantly, these compounds potently inhibit clin. relevant D816V mutations of c-KIT in biochem. and cellular studies.
Journal of Medicinal Chemistry published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Quality Control of 757978-19-1.
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