Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 882562-40-5, is researched, SMILESS is ClC1=NC(C2=CN(C3=C2C=CC=C3)S(=O)(=O)C2=CC=CC=C2)=C(Cl)C=N1, Molecular C18H11Cl2N3O2SJournal, Article, Journal of Medicinal Chemistry called Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR), Author is Ward, Richard A.; Anderton, Mark J.; Ashton, Susan; Bethel, Paul A.; Box, Matthew; Butterworth, Sam; Colclough, Nicola; Chorley, Christopher G.; Chuaqui, Claudio; Cross, Darren A. E.; Dakin, Les A.; Debreczeni, Judit E.; Eberlein, Cath; Finlay, M. Raymond V.; Hill, George B.; Grist, Matthew; Klinowska, Teresa C. M.; Lane, Clare; Martin, Scott; Orme, Jonathon P.; Smith, Peter; Wang, Fengjiang; Waring, Michael J., the main research direction is EGFR activating gatekeeper mutant covalent inhibitor SAR.Synthetic Route of C18H11Cl2N3O2S.
A novel series of small-mol. inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib. Our reported compounds also show selectivity over wild-type EGFR. Guided by mol. modeling, this series was evolved to target a cysteine residue in the ATP binding site via covalent bond formation and demonstrates high levels of activity in cellular models of the double mutant form of EGFR. In addition, these compounds show significant activity against the activating mutations, which gefitinib and erlotinib target and inhibition of which gives rise to their observed clin. efficacy. A glutathione (GSH)-based assay was used to measure thiol reactivity toward the electrophilic functionality of the inhibitor series, enabling both the identification of a suitable reactivity window for their potency and the development of a reactivity quant. structure-property relationship (QSPR) to support design.
In some applications, this compound(882562-40-5)Synthetic Route of C18H11Cl2N3O2S is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.
Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem