Singh, Pankaj Kumar published the artcileStructure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC, Recommanded Product: 3-Chlorobenzylchloride, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(13), 1565-1571, database is CAplus and MEDLINE.
Secondary acquired mutant EGFR (L858R-T790M) overexpressed NSCLC forms one of the prevalent form of resistant NSCLC. Another subset of resistant NSCLC includes amplified cMET in mutant EGFR derived tumors. Thus, in continuation to our previous work on these two major targets of resistant NSCLC, i.e., EGFR (L858R-T790M) and cMET, we are hereby reporting reversible inhibitors of these kinases. Out of 11 lead mols. reported in our previous study, we selected triazolo-pyrimidone (BAS 09867482) scaffold for further development of small mol. dual and reversible inhibitors. Analogs of lead with different substituents on the side ring were sketched and docked in both the target kinases, followed by mol. dynamic simulations. Analogs maintaining hydrophobic interaction with M790 in secondary acquired mutant EGFR (L858R-T790M) were selected and duly synthesized. In vitro biochem. evaluation of these mols. against EGFR (L858R-T790M) and cMET kinase, along with EGFR (L858R) kinase disclosed that three mols. were having significant dual kinase inhibitory potential with IC50 values well below 100 nM. Further, in vitro anti-proliferative assay against three cell lines (A549, A431 and H460) was performed. Out of all, two compounds were having significant potency against these cell lines.
Bioorganic & Medicinal Chemistry Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C6H13BO3, Recommanded Product: 3-Chlorobenzylchloride.
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https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics