1261566-52-2Relevant academic research and scientific papers
Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors
Bardiot, Dorothée,Koukni, Mohamed,Smets, Wim,Carlens, Gunter,McNaughton, Michael,Kaptein, Suzanne,Dallmeier, Kai,Chaltin, Patrick,Neyts, Johan,Marchand, Arnaud
supporting information, p. 8390 - 8401 (2018/09/25)
3-Acyl-indole derivative 1 was identified as a novel dengue virus (DENV) inhibitor from a DENV serotype 2 (DENV-2) phenotypic antiviral screen. Extensive SAR studies led to the discovery of new derivatives with improved DENV-2 potency as well as activity in nanomolar to micromolar range against the other DENV serotypes. In addition to the potency, physicochemical properties and metabolic stability in rat and human microsomes were improved during the optimization process. Chiral separation of the racemic mixtures showed a clear preference for one of the two enantiomers. Furthermore, rat pharmacokinetics of two compounds will be discussed in more detail, demonstrating the potential of this new series of pan-serotype-DENV inhibitors.
Novel histone deacetylase 8 ligands without a zinc chelating group: Exploring an 'upside-down' binding pose
Vaidya, Aditya Sudheer,Neelarapu, Raghupathi,Madriaga, Antonett,Bai, He,Mendonca, Emma,Abdelkarim, Hazem,Van Breemen, Richard B.,Blond, Sylvie Y.,Petukhov, Pavel A.
, p. 6621 - 6627 (2013/01/14)
A novel series of HDAC8 inhibitors without a zinc-chelating hydroxamic acid moiety is reported. Photoaffinity labeling and molecular modeling studies suggest that these ligands are likely to bind in an 'upside-down' fashion in a secondary binding site pro
PYRAZOLYL QUINAZOLINE KINASE INHIBITORS
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, (2011/11/13)
The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
