alexa Structure-activity relationship study of novel tissue transglutaminase inhibitors.


Medicinal Chemistry

Author(s): Duval E, Case A, Stein RL, Cuny GD

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Abstract Thieno[2,3-d]pyrimidin-4-one acylhydrazide derivatives were discovered as moderately potent inhibitors of TGase 2 (tissue transglutaminase) utilizing a fluorescence-based assay that measured TGase 2 catalyzed incorporation of the dansylated Lys derivative alpha-N-Boc-Lys-CH(2)-CH(2)-dansyl into the protein substrate N,N-dimethylated-casein. A SAR study revealed that the acylhydrazide thioether side-chain and the thiophene ring were critical to inhibitory activity. This article was published in Bioorg Med Chem Lett and referenced in Medicinal Chemistry

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