81677-61-4Relevant articles and documents
Small molecule macroarray construction via Ugi four-component reactions
Lin, Qi,O'Neill, Jennifer C.,Blackwell, Helen E.
, p. 4455 - 4458 (2005)
(Chemical Equation Presented) We report the construction of small molecule macroarrays via Ugi four-component reactions on planar cellulose supports. Array synthesis was enabled by the development of a high efficiency photocleavable linker system and the
Synthesis and evaluation of an enantiomerically enriched bifunctional chelator for 64Cu-based positron emission tomography (PET) imaging
Chong, Hyun-Soon,Sun, Xiang,Zhong, Yongliang,Bober, Kamil,Lewis, Michael R.,Liu, Dijie,Ruthengael, Varyanna C.,Sin, Inseok,Kang, Chi Soo
, p. 1305 - 1313 (2014/03/21)
We report the synthesis and evaluation of an enantiomerically enriched bifunctional chelator, (S)-C-NE3TA. The bifunctional chelator was efficiently prepared by regioselective and stereoselective ring opening of an aziridinium ion. The new chiral chelator instantly and almost completely bound to 64Cu at room temperature. The corresponding 64Cu- radiolabeled complex remained intact in human serum for 48 h without any measurable transchelation and was tolerant to a rigorous EDTA challenge for 24 h. The 64Cu-radiolabeled (S)-C-NE3TA complex was stable in mice and produced an excellent biodistribution profile. The results of the in vitro and in vivo evaluations indicate that the new optically active chelator is a promising candidate for PET imaging applications. We report an enantiomerically enriched bifunctional ligand in the NE3TA series for the first time. The chelator instantly bound to 64Cu to form a complex that was stable in vitro and in vivo and possesses great promise for use in targeted positron emission topography (PET) imaging. Copyright
Indole nitriles
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Page 123, (2010/02/06)
Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.