Bryan McKibben

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Until recently, the characterization of adenosine A(2B) receptors has been hampered by the lack of high affinity radioligands. This study describes the synthesis and in vitro characterization of the radiolabeled derivative of OSIP339391, a novel, potent, and selective pyrrolopyrimidine A(2B) antagonist. OSIP339391 had a selectivity of greater than 70-fold(More)
Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system(More)
The CXCL12/CXCR4 axis is involved in many cellular responses for host homeostasis, and malfunction of this signaling pathway is associated with a variety of diseases. It is now known that CXCL12 also binds to another newly identified chemokine receptor, CXCR7, which does not couple with a G-protein. CXCR7 can form homodimers, or heterodimers with CXCR4, and(More)
A general, scalable, and highly diastereoselective aziridination of N-tert-butanesulfinyl ketimino esters is described. The methodology has been utilized to provide straightforward access to previously unobtainable, biologically relevant α-quaternary amino esters and derivatives starting from readily available precursors.
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