Tang, Guanghui; Liu, Lihong; Wang, Xueying; Pan, Zhengying published the article 《Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk)》. Keywords: pyrrolo pyrimidine derivative preparation Itk kinase inhibitor cancer; 7H-pyrrolo[2,3-d]pyrimidine; Covalent inhibitor; Itk; Selectivity.They researched the compound: Boc-D-Prolinol( cas:83435-58-9 ).Synthetic Route of C10H19NO3. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:83435-58-9) here.
Interleukin-2-inducible T-cell kinase (Itk) plays an important role in multiple signal transduction pathways in T and mast cells, and is a potential drug target for treating inflammatory diseases, autoimmune diseases, and T cell leukemia/lymphoma. Herein, we describe the discovery of a series of covalent Itk inhibitors based on the 7H-pyrrolo[2,3-d]pyrimidine scaffold. Placing an appropriate substitution group at a hydration site of the ATP binding pocket of Itk and using a saturated heterocyclic ring as a linker to the reactive group were crucial for selectivity. The optimized compound 9 showed potent activity against Itk, excellent selectivity for Itk over Btk and other structurally related kinases, inhibition of phospholipase C-γ1 (PLC-γ1) phosphorylation in cells, and anti-proliferative effects against multiple T leukemia/lymphoma cell lines. Compound 9 can serve as a valuable compound for further determination of functions of Itk.
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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica