Chan, Bryan K. published the artcileDiscovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor, Quality Control of 1260672-72-7, the publication is Journal of Medicinal Chemistry (2016), 59(19), 9080-9093, database is CAplus and MEDLINE.
Inhibitors targeting the activating mutants of the epidermal growth factor receptor (EGFR) have found success in the treatment of EGFR mutant pos. nonsmall-cell lung cancer. A secondary point mutation (T790M) in the inhibitor binding site has been linked to the acquired resistance against those first generation therapeutics. Herein, the authors describe the lead optimization of a series of reversible, pan-mutant (L858R, del746-750, T790M/L858R, and T790M/del746-750) EGFR inhibitors. By use of a noncovalent double mutant (T790M/L858R and T790M/del746-750) selective EGFR inhibitor I as a starting point, activities against the single mutants (L858R and del746-750) were introduced through a series of structure-guided modifications. The in vitro ADME-PK properties of the lead mols. were further optimized through a number of rational structural changes. The resulting inhibitor II exhibited excellent cellular activity against both the single and double mutants of EGFR, demonstrating target engagement in vivo and ADME-PK properties that are suitable for further evaluation. The reversible, noncovalent inhibitors described complement the covalent pan-mutant EGFR inhibitors that have shown encouraging results in recent clin. trials.
Journal of Medicinal Chemistry published new progress about 1260672-72-7. 1260672-72-7 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Iodide, name is 6-Chloro-3-iodo-1H-pyrazolo[4,3-c]pyridine, and the molecular formula is C6H3ClIN3, Quality Control of 1260672-72-7.
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https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com