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Effects of Surfactant and Polymer on Thermodynamic Solubility and Solution Stability of Carbamazepine–Cinnamic Acid Cocrystal
This study was aimed at evaluating the solubility and solution stability of a cocrystal form of carbamazepine with cinnamic acid in the presence of...
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Differential Scanning Calorimetry Study of the Ibuprofen–Nicotinamide Binary Disperse System and the Anti-Inflammatory Activity of One of Its Secondary Eutectics
Phase equilibria in the solid disperse system ibuprofen–nicotinamide were studied by differential scanning calorimetry (DSC). It was established that...
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The Antidiarrheal Activity of Octacosanol is Mediated by the Possible Participation of α2 Adrenoreceptors
Senna septemtrionalis (Viv.) H.S. Irwin & Barneby, Fabaceae, is a shrub used for treating asthma, diarrhea, and sore throat. This work evaluated for...
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Transcriptome analysis of an AKT inhibitor-resistant endometrial cancer cell line
BackgroundDrug resistance in endometrial cancer (EC) is a serious problem and a barrier to improving prognosis. The PI3K/AKT/mTOR pathway is highly...
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Design, Synthesis and Biological Evaluation of Amide Derivatives of Thiazolo[5,4-d]Pyrimidines as Cytotoxicity Agents for Human Cancer Cell Lines
We have designed and synthesized a new series of amide derivatives of thiazolo[5,4- d ]pyrimidines ( 10a-j ) and their structures were characterized by 1 H...
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Engineering of Dihydroquercetin Crystals
Dihydroquercetin (DHQ) is a commercially available bioflavonoid with a wide range of pharmacological activity. The low water solubility at room...
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Challenges and opportunities of develo** small-molecule therapies for age-related macular degeneration
Age-related macular degeneration (AMD) is the leading cause of vision loss in senior adults. The disease can be categorized into two types: wet AMD...
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Strategies for Solubility Enhancement of Anthelmintics (Review)
Most drug substances are poorly soluble in water so that their efficacies must be improved by increasing the dosage, which not only creates economic...
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Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation
A supersaturating self-emulsifying drug delivery system (S-SEDDS) was prepared and evaluated for enhanced dissolution of celecoxib (CXB), a poorly...
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Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics
Aberrant activation of Raf signaling pathway is frequently found in various human tumors, it has been considered as distinct and promising molecular...
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Sesquiterpene Lactones from Stizolophus balsamita and Their Biological Activity
Four sesquiterpene lactones with the germacrane structure were isolated from the aerial part of Stizolophus balsamita . X-ray structure analyses...
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Receptor-Binding Sites
It is increasingly clear that both transient and long-lasting interactions between biomacromolecules and their molecular partners are the most...
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Chemistry and biology of ras farnesyltransferase
Mutated forms of ras are found in many human tumors and the rate of incidence is significantly higher in colon and pancreatic cancers. The protein...
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Farnesyltransferase Inhibitors
Oncogenic ras mutations and aberrant Ras function are important in many human tumors, so blocking the activity of oncogenic Ras has been a...
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Structure-based drug design (SBDD): Every structure tells a story...
In this article we report how protein-ligand X-ray structures can be used to identify and develop new drug candidates. The structure-based drug...