Suppression of Initial Degradation via an Interfacial Charge-Induced Overshooting Effect in Solution-Processed Organic Light-Emitting Diodes.

As the chemical stability of organic materials in organic light-emitting diodes (OLEDs) greatly impacts devices' lifetime, a thoughtful and advanced design of materials and device structures is necessary. In our work, we have achieved lifetime enhancement at its initial stage for solution-processed OLEDs. This improvement was realized through the implementation of a double electron transporting layer (dETL) composed of 2-[4-(9,10-dinaphthalen-2-yl-anthracen-2-yl)-phenyl]-1-phenyl-1H-benzoimidazole (ET) and hydroxyquinolinolato-lithium (Liq).

Organic Phototransistor with Light-Induced Contact Modulation and Sensitivity Enhancement Using a C/C:TAPC Hybrid Channel.

Organic phototransistors (OPTs) are attracting a significant degree of interest as devices that have the potential to play multiple roles, including light sensing, signal amplification, and switching for addressing when they are used for matrix arrays. However, it has been challenging to realize OPTs that can perform all of these roles simultaneously at a sufficient performance level because the channel materials with high carrier mobility often exhibit relatively low photoabsorption. In this work, we propose OPTs with a hybrid bilayer channel consisting of a neat C layer and a bulk-heterojunction layer of C and 1,1-bis(4-bis(4-methyl-phenyl)-amino-phenyl)-cyclohexane (TAPC) as a possible solution to this issue.

PCW-A1001, AI-assisted design approach to design a selective inhibitor for FLT-3(D835Y) in acute myeloid leukemia.

Treating acute myeloid leukemia (AML) by targeting FMS-like tyrosine kinase 3 (FLT-3) is considered an effective treatment strategy. By using AI-assisted hit optimization, we discovered a novel and highly selective compound with desired drug-like properties with which to target the FLT-3 (D835Y) mutant. In the current study, we applied an AI-assisted design approach to identify a novel inhibitor of FLT-3 (D835Y).

Discovery of BET specific bromodomain inhibitors with a novel scaffold.

Bromodomain and extra-terminal domain (BET) proteins have been considered as potent candidates for anti-cancer drug development. As epigenetic readers, they modulate gene expression by recognizing acetylated lysine residues on histones. Therefore, the pharmacological inhibition of BET proteins has been extensively studied.

PCW-1001, a Novel Pyrazole Derivative, Exerts Antitumor and Radio-Sensitizing Activities in Breast Cancer.

As pyrazole and its derivatives have a wide range of biological activities, including anticancer activity, the design of novel pyrazole derivatives has emerged as an important research field. This study describes a novel pyrazole derivative that exerts antitumor and radiosensitizing activities in breast cancer both and . We synthesized a novel pyrazole compound N,N-dimethyl-N'-(3-(1-(4-(trifluoromethyl)phenyl)-1H-pyrazol-4-yl)phenyl)azanesulfonamide (PCW-1001) and showed that it inhibited several oncogenic properties of breast cancer both and .

A visible-light phototransistor based on the heterostructure of ZnO and TiO with trap-assisted photocurrent generation.

Visible-light phototransistors have been fabricated based on the heterojunction of zinc oxide (ZnO) and titanium oxide (TiO). A thin layer of TiO was deposited onto the spin-coated ZnO film atomic layer deposition (ALD). The electrical characteristics of the TiO layer were optimized by controlling the purge time of titanium isopropoxide (TTIP).

Synthesis and Structure-Activity Relationships of Aristoyagonine Derivatives as Brd4 Bromodomain Inhibitors with X-ray Co-Crystal Research.

Epigenetic regulation is known to play a key role in progression of anti-cancer therapeutics. Lysine acetylation is an important mechanism in controlling gene expression. There has been increasing interest in bromodomain owing to its ability to modulate transcription of various genes as an epigenetic 'reader.

Degrasyn exhibits antibiotic activity against multi-resistant Staphylococcus aureus by modifying several essential cysteines.

Degrasyn inhibits deubiquitination enzymes and has anti-cancer activity. We here show that it also exhibits antimicrobial activity against multi-resistant Staphylococcus aureus. Structure activity relationship studies demonstrate an important role of the electrophilic α-cyanoacrylamide moiety as a Michael acceptor.

Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.

Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of hit anthraquinone led to the identification of a new series of allosteric PDK4 inhibitors. Among this series, compound 8c showed promising in vitro activity with an IC value of 84 nM.

A Chemical Disruptor of the ClpX Chaperone Complex Attenuates the Virulence of Multidrug-Resistant Staphylococcus aureus.

The Staphylococcus aureus ClpXP protease is an important regulator of cell homeostasis and virulence. We utilized a high-throughput screen against the ClpXP complex and identified a specific inhibitor of the ClpX chaperone that disrupts its oligomeric state. Synthesis of 34 derivatives revealed that the molecular scaffold is restrictive for diversification, with only minor changes tolerated.

Design, synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists.

A series of N-methoxyamide derivatives was identified and evaluated as GPR119 agonists. Several N-methoxyamides with thienopyrimidine and pyridine scaffolds showed potent GPR119 agonistic activities. Among them, compound 9c displayed good in vitro activity and potency.

Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists.

A series of thienopyrimidine derivatives was synthesized and evaluated for their GPR119 agonistic ability. Several thienopyrimidine derivatives containing R(1) and R(2) substituents displayed potent GPR119 agonistic activity. Among them, compound 5d, which is a prototype, showed good in vitro activity with an EC50 value of 3 nM and human and rat liver microsomal stability.