22276-16-0Relevant articles and documents
Discovery of 1,2,4-oxadiazole derivatives as a novel class of noncompetitive inhibitors of 3-hydroxykynurenine transaminase (HKT) from Aedes aegypti
Guido, Rafael V. C.,Leal, Laylla L. L.,Maciel, Larissa G.,Oliveira, Andrew A.,Rom?o, Tatiany P.,Silva-Filha, Maria Helena N. L.,Soares, Thereza A.,dos Anjos, Janaína V.
, (2020/01/03)
The mosquito Aedes aegypti is the vector of arboviruses such as Zika, Chikungunya, dengue and yellow fever. These infectious diseases have a major impact on public health. The unavailability of effective vaccines or drugs to prevent or treat most of these
PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
-
Paragraph 00179, (2013/04/13)
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4- oxadiazoles as a new series of apoptosis inducers and potential anticancer agents
Zhang, Han-Zhong,Kasibhatla, Shailaja,Kuemmerle, Jared,Kemnitzer, William,Ollis-Mason, Kristin,Qiu, Ling,Crogan-Grundy, Candace,Tseng, Ben,Drewe, John,Cai, Sui Xiong
, p. 5215 - 5223 (2007/10/03)
We have identified 5-(3-chlorothiophen-2-yl)-3-(4-trifluoromethylphenyl)-1, 2,4-oxadiazole (1d) as a novel apoptosis inducer through our caspase- and cell-based high-throughput screening assay. Compound 1d has good activity against several breast and colorectal cancer cell lines but is inactive against several other cancer cell lines. In a flow cytometry assay, treatment of T47D cells with 1d resulted in arrest of cells in the G1 phase, followed by induction of apoptosis. SAR studies of Id showed that the 3-phenyl group can be replaced by a pyridyl group, and a substituted five-member ring in the 5-position is important for activity. 5-(3-Chlorothiophen-2-yl)-3-(5- chloropyridin-2-yl)-1,2,4-oxadiazole (41) has been found to have in vivo activity in a MX-1 tumor model. Using a photoaffinity agent, the molecular target has been identified as TIP47, an IGFII receptor binding protein. Therefore, our cell-based chemical genetics approach for the discovery of apoptosis inducers can identify potential anticancer agents as well as their molecular targets.