Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck: Synthesis, SAR, and in Vivo Anti-Inflammatory Activity was written by DiMauro, Erin F.;Newcomb, John;Nunes, Joseph J.;Bemis, Jean E.;Boucher, Christina;Buchanan, John L.;Buckner, William H.;Cee, Victor J.;Chai, Lilly;Deak, Holly L.;Epstein, Linda F.;Faust, Ted;Gallant, Paul;Geuns-Meyer, Stephanie D.;Gore, Anu;Gu, Yan;Henkle, Brad;Hodous, Brian L.;Hsieh, Faye;Huang, Xin;Kim, Joseph L.;Lee, Josie H.;Martin, Matthew W.;Masse, Craig E.;McGowan, David C.;Metz, Daniela;Mohn, Deanna;Morgenstern, Kurt A.;Oliveira-dos-Santos, Antonio;Patel, Vinod F.;Powers, David;Rose, Paul E.;Schneider, Stephen;Tomlinson, Susan A.;Tudor, Yan-Yan;Turci, Susan M.;Welcher, Andrew A.;White, Ryan D.;Zhao, Huilin;Zhu, Li;Zhu, Xiaotian. And the article was included in Journal of Medicinal Chemistry in 2006.Related Products of 133232-56-1 This article mentions the following:
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. Screening of our kinase-preferred collection identified aminoquinazoline I as a potent, nonselective inhibitor of Lck and T cell proliferation. In this report, we describe the synthesis and structure-activity relationships of a series of novel aminoquinazolines possessing in vitro mechanism-based potency. Two optimized, orally bioavailable compounds exhibit antiinflammatory activity (ED50 of 22 and 11 mg/kg, resp.) in the anti-CD3-induced production of interleukin-2 (IL-2) in mice. In the experiment, the researchers used many compounds, for example, 3-Iodo-2-methylbenzoic acid (cas: 133232-56-1Related Products of 133232-56-1).
3-Iodo-2-methylbenzoic acid (cas: 133232-56-1) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Related Products of 133232-56-1
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com