The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: tert-Butyl 2-cyanoacetate, is researched, Molecular C7H11NO2, CAS is 1116-98-9, about Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists, the main research direction is cancer CXCR2 antagonist CXCL8 ERK beta arrestin phosphorylation recruitment; CXCL8; CXCR2; GPCR; Thioureidothiophene; cAMP; β-arrestin.Quality Control of tert-Butyl 2-cyanoacetate.
The C-X-C motif ligand 8 and C-X-C chemokine receptor 2 (CXCL8-CXCR2) axis is involved in pathogenesis of various diseases including inflammation and cancers. Various CXCR2 antagonists are under development for several diseases. Our previous high-throughput cell-based assay specific for CXCR2 has identified a pyrimidine-based compound CX797 acting on CXCR2 down-stream signaling. A lead optimization campaign through scaffold-hopping strategy led to a series of 2-thioureidothiophene-3-carboxylates (TUTP) as novel CXCR2 antagonists. Structure-activity relationship study of TUTPs led to the identification of compound 52(I) that significantly inhibited CXCR2-mediated β-arrestin recruitment signaling (IC50 = 1.1±0.01 μM) with negligible effect on CXCL8-mediated cAMP signaling and calcium flux. Similar to the known CXCR2 antagonist SB265610, compound 52 inhibited CXCL8-CXCR2 induced phosphorylation of ERK1/2. TUTP compounds also inhibited CXCL8-mediated cell migration and showed synergy with doxorubicin in ovarian cancer cells, thereby supporting TUTPs as promising compounds for cancer treatment.
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Reference:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem