49855-91-6Relevant articles and documents
COMPOUNDS
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Paragraph 0971-0974, (2021/06/26)
Compounds of general formula (I) wherein R1, R2, R3, R4 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and
Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity
Satyanarayana, Mavurapu,Kim, Young-Ah,Rzuczek, Suzanne G.,Pilch, Daniel S.,Liu, Angela A.,Liu, Leroy F.,Rice, Joseph E.,LaVoie, Edmond J.
scheme or table, p. 3150 - 3154 (2010/09/10)
A series of 24-membered macrocyclic hexaoxazoles containing one or two aminoalkyl substituents was synthesized and evaluated for cytotoxicity and for their ability to selectively stabilize G-quadruplex DNA and RNA. The most cytotoxic analog 4a, with IC50 values of 25 and 130 nM using KB3-1 and RPMI 8402 cells, is efficacious in vivo in athymic nude mice with a human tumor xenograft from the breast cancer cell line MDA-MB-435.
Synthesis and evaluation of peptidic maleimides as transglutaminase inhibitors
Halim, Dany,Caron, Karine,Keillor, Jeffrey W.
, p. 305 - 308 (2007/10/03)
A series of novel transglutaminase inhibitors was prepared, based on the scaffold of a commonly used peptide substrate and bearing an electrophilic maleimide group. These compounds were evaluated in vitro and shown to lead to irreversible inactivation of tissue transglutaminase. Comparison with inhibitors studied previously provides insight into the steric environment of the enzyme active site.