49855-91-6Relevant academic research and scientific papers
BENZODIAZOLIUM COMPOUNDS AS ENAC INHIBITORS
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Page/Page column 157-158, (2018/06/12)
Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respirator
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.
THERAPEUTIC COMPOUNDS
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Page/Page column 58, (2009/03/07)
The invention provides compounds of formula (I) wherein A, B, R1, F, G, n, n' and the dotted line have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.
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.
N(ω)-nitroarginine-containing dipeptide amides. Potent and highly selective inhibitors of neuronal nitric oxide synthase
Huang, Hui,Martasek, Pavel,Roman, Linda J.,Masters, Bettie Sue Siler,Silverman, Richard B.
, p. 3147 - 3153 (2007/10/03)
Selective inhibition of the isoforms of nitric oxide synthase (NOS) could be therapeutically useful in the treatment of certain disease states arising from the overproduction of nitric oxide (NO). Recently, we reported the dipeptide methyl ester, D-Phe-D-
Modification of receptor selectivity and functional activity of cyclic cholecystokinin analogues
Amblard, Muriel,Rodriguez, Marc,Lignon, Marie-Francoise,Galas, Marie-Christine,Bernad, Nicole,Aumelas, Andre,Martinez, Jean
, p. 171 - 180 (2007/10/03)
We reported earlier on the synthesis and biological activity at the CCK-B receptor of cyclized derivatives of CCK. These peptides, in which the positions 28 and 31 were replaced by lysine residues, were bridged by a succinyl moiety. To determine the importance of the nature and size of the cyclic structure, cyclic analogues were synthesized in which: (i) the lysine residues were replaced by ornithine and diaminobutyric acid and (ii) the succinic moiety was replaced by a malonic, adipic and glutaric moiety. They were tested For their ability to inhibit the specific binding of 125I-BH-CCK-8 to CCK receptors in rat pancreatic acini and guinea pig brain membranes. They were also evaluated for their ability to stimulate amylase secretion from rat pancreatic acini. The potency and selectivity of these analogues were compared with those obtained with CCK-4 and compound JIMV320, a potent and selective CCK-B receptor ligand synthesized earlier in our laboratory.
