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Design and Synthesis of a Series of Piperazine‐1‐carboxamidine Derivatives with Antifungal Activity Resulting from Accumulation of Endogenous Reactive Oxygen Species
TLDR
This study screened a library of 500 compounds for fungicidal activity via induction of endogenous reactive oxygen species (ROS) accumulation and could link the fungicidal mode of action of the piperazine‐1‐carboxamidine derivatives to the accumulation of endogenous ROS. Expand
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.
TLDR
The optimization of imidazo [1,2-a] pyrazines is described, which allow us to identify compound 14 (ETP-46321), with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. Expand
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
TLDR
A novel series of imidazo[1,2-a]pyrazines as PI3K inhibitors is described as an important target for cancer therapeutics due to the deregulation of its signaling pathway in a wide variety of human cancers. Expand
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.
TLDR
The rapid identification of ETP-46992, within 2-aminocarbonyl imidazo [1,2-a] pyrazine series, with suitable pharmacokinetic (PK) properties that allows the establishment of mechanism of action and efficacy in vivo studies is described. Expand
Callosal agenesis, chorioretinal lacunae, absence of infantile spasms, and normal development: Aicardi syndrome without epilepsy?
TLDR
A case of Aicardi syndrome is described in a female aged 24 months, whose psychomotor and language development were normal for age, and Magnetic resonance imaging showed complete agenesis of the corpus callosum and ophthalmoscopy revealed chorioretinal lacunae in the left eye. Expand
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.
TLDR
A further exploration of the lead PI3K inhibitor ETP-46321 is reported by the application of a conformational restriction strategy and novel tricyclic imidazo[1,2-a]pyrazine derivatives asPI3K inhibitors are synthesized. Expand
[Hodgkin's disease. Etiopathogenic role of Epstein-Barr virus in Tarragona].
TLDR
EBV is associated with 40.8% of HD in area of Tarragona, and was higher, but not significant, in mixed cellularity, and significant higher in patients over 55 years old. Expand
Identification of novel PI3K inhibitors through a scaffold hopping strategy.
TLDR
A scaffold hopping strategy, including intellectual property availability assessment, was successfully applied for the discovery of novel PI3K inhibitors that showed good in vitro potency and selectivity, and proved to inhibit potently the phosphorylation of AKTSer473 in cells. Expand
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