Discovery of Potent and Selective SH2 Inhibitors of the Tyrosine Kinase ZAP-70 was written by Vu, Chi B.;Corpuz, Evelyn G.;Merry, Taylor J.;Pradeepan, Selvaluxmi G.;Bartlett, Catherine;Bohacek, Regine S.;Botfield, Martyn C.;Eyermann, Charles J.;Lynch, Berkley A.;MacNeil, Ian A.;Ram, Mary K.;Van Schravendijk, Marie Rose;Violette, Shelia;Sawyer, Tomi K.. And the article was included in Journal of Medicinal Chemistry in 1999.Application In Synthesis of 2-(4-Bromophenyl)-N-hydroxyacetimidamide The following contents are mentioned in the article:
A series of 1,2,4-oxadiazole analogs has been shown to be potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70, a potential therapeutic target for immune suppression. These compounds typically are 200-400-fold more potent than the native, monophosphorylated tetrapeptide sequences. When compared with the high-affinity ΞΆ-1-ITAM peptide (Ac-NQL-pYNELNLGRREE-pYDVLD-NH2, wherein pY refers to phosphotyrosine) some of the best 1,2,4-oxadiazole analogs are approx. 1 order of magnitude less active. This series of compounds displays an unprecedented level of selectivity over the closely related tyrosine kinase Syk, as well as other SH2-containing proteins such as Src and Grb2. Gel shift studies using a protein construct consisting only of C-terminal ZAP-70 SH2 demonstrate that these compounds can effectively engage this particular SH2 domain. This study involved multiple reactions and reactants, such as 2-(4-Bromophenyl)-N-hydroxyacetimidamide (cas: 422560-40-5Application In Synthesis of 2-(4-Bromophenyl)-N-hydroxyacetimidamide).
2-(4-Bromophenyl)-N-hydroxyacetimidamide (cas: 422560-40-5) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Application In Synthesis of 2-(4-Bromophenyl)-N-hydroxyacetimidamide
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary