Results 81 to 90 of about 666,519 (246)
Rationally designed naphthyl pyrazino‐pyrido‐pyrimidinones 3 and 4 inhibited 85%–94% of cancer cell growth. Compound 4 exhibited IC50 = 7.8–12.8 µM with tumor selectivity. Both induced G1 arrest and modulated ULK1, STAT3, alpha‐serine/protein kinase B (AKT), and autophagy via phosphoinositide 3‐kinase/mammalian target of rapamycin (PI3K/mTOR ...
Marcelo F. Marchiori +6 more
wiley +1 more source
In recent years, pharmaceutical cocrystal has become a hot field in drug development, which improves the solubility, stability, and bioavailability of drugs.
Haofei Sun +7 more
doaj +1 more source
De Novo Design and Synthesis of Novel Benzoxazinone Derivatives Targeting Dihydroxyacid Dehydratase
ABSTRACT Dihydroxyacid dehydratase (DHAD), a key enzyme in the branched‐chain amino acid (BCAA) synthesis pathway, is a promising herbicide target. Currently, no commercial herbicides target DHAD, and no inhibitors are in development. Structural analysis suggests that coordination with iron–sulfur clusters and hydrophobic interactions with Tyr215 and ...
Bo He +7 more
wiley +1 more source
Charge‐transfer coassembly enables precise control over the dynamic aggregation process, resulting in morphology evolution from amorphous aggregates to rod‐like and needle‐like microcrystals, accompanied by a significant fluorescence enhancement. This strategy yields widely tunable solid‐state emission from green to orange‐red, unveiling fundamental ...
Huiting Mao +7 more
wiley +1 more source
A Review on Pharmaceutical Cocrystals
Pharmaceutical cocrystals are crystalline materials composed of two or more different molecules, at least one being an active pharmaceutical ingredient (API), in a fixed stoichiometric ratio, held together by non-covalent interactions.Cocrystal can be prepared by cocrystallization method.
Samina Sameer +3 more
openaire +1 more source
A Proteochemometric Model for Ligands of the SLC5 Transporter Family
A novel proteochemometric model was developed to predict the activity and selectivity of SLC5 family inhibitors. The model's performance was validated using 10‐fold cross‐validation on publicly available datasets achieving Q2 = 0.79 and MSE < 0.32. Detailed analysis of the results enabled the identification of a new, previously unrecognized selectivity‐
Martin Juhás, Gerhard Ecker
wiley +1 more source
Febuxostat (FB) is a poorly water-soluble drug that belongs to BCS class II. The drug is employed for the treatment of inflammatory disease arthritis urica (gout), and the free base, FB form-A, is most preferred for drug formulation.
Ji-Hun An +9 more
doaj +1 more source
Pharmaceutical Cocrystal of Ethyl p-Methoxycinnamate: Formulation and Characterization
Ethyl p-methoxycinamate (EPMC) is a compound derived from kencur (Kaemferia galanga) and has a pharmacological effect as an antiinflammatory. EPMC has poorly water solubility and need to be modified to increase its solubility.
Revika Rachmaniar +5 more
semanticscholar +1 more source
Dissolution rate of ciprofloxacin and its cocrystal with resorcinol
The synthesis of cocrystals is presented as an alternative to improve the properties of active pharmaceutical ingredients, especially those related to solubility and dissolution rate.
Clara Ràfols +5 more
doaj +1 more source
Recent advances in pharmaceutical cocrystals of theophylline
AbstractCurrently, cocrystallization is a promising strategy for tailoring the physicochemical properties of active pharmaceutical ingredients. Theophylline, an alkaloid and the most primary metabolite of caffeine, is a readily available compound found in tea and coffee.
Yanxiao Jia +7 more
openaire +3 more sources

