The predictive value of nontraditional lipid parameters for intracranial and extracranial atherosclerotic stenosis: a hospital-based observational study in China.

Background: Ischemic strokes are primarily caused by intracranial and extracranial atherosclerotic stenosis. Nontraditional lipid parameters broaden traditional lipid profiles, better reflect the metabolism and interaction between different lipid components, and optimize the predictive ability of lipid profiles for atherosclerotic diseases. This research was carried out to investigate the predictive value of nontraditional lipid parameters for intracranial or extracranial atherosclerotic stenosis.

The role of natural organic matter in the silver release from sludge generated from coagulation of wastewater spiked with silver nanoparticles.

Sludge is an integral part in the migration pathway of silver nanoparticles (AgNPs) from manufacture to the terrestrial environment. However, the detailed information on the role of natural organic matters (NOMs) remains limited. In this study, the sludge generated from coagulation of wastewater spiked with AgNPs (denoted as sludge) was taken as the model.

Design, synthesis, and in vitro antitumor activity of 6-aryloxyl substituted quinazoline derivatives.

Quinazoline derivatives are a class of important antitumor drugs known as small molecule inhibitors that include epidermal growth factor receptor (EGFR) inhibitors. Based on the structure of poziotinib, a series of 6-aryloxyl substituted quinazoline derivatives were designed and synthesized. The in vitro antitumor activities of the compounds were evaluated by the 3-(4,5-dimethyl-thiazol-2-yl) 2,5-diphenyltetrazolium bromide (MTT) method using the human gastric cancer N87 (HER2), nonsmall-cell lung cancer H1975 (EGFR), and A549 (EGFR) cell lines.

The Synthesis, Structural Modification and Mode of Anticancer Action of Evodiamine: A Review.

Background: Finding novel antitumor reagents from naturally occurring alkaloids is a widely accepted strategy. Evodiamine, a tryptamine indole alkaloid isolated from Evodia rutaecarpa, has a wide range of biological activities, such as anti-tumor, anti-inflammation, and anti-bacteria. Hence, research on the structural modification of evodiamine will facilitate the discovery of new antitumor drugs.

The Design, Synthesis and Evaluation of Rho-kinase Inhibitory Activity of 4-aryl-thiazole-2-amines.

Rho-associated kinases (ROCK) are a class of serine/threonine kinases that play important roles in various biological processes. ROCK are becoming attractive targets for drug designing. A novel scaffold was designed according to molecular hybridization strategy, then a series of 4-aryl-5-aminomethyl-thiazole-2-amines were synthesized, and their inhibitory activities on ROCK were screened by enzyme-linked immunosorbent assay (ELISA).

Design, synthesis, and biological evaluation of urea-based ROCK2 inhibitors.

A series of urea-based ROCK2 inhibitors were design and synthesized. The inhibitory activity on ROCK2 was screened by enzyme-linked immunosorbent assay (ELISA). The study results showed that the urea derivatives exhibited certain ROCK2 inhibitory activity.

Speciation, controlling steps and pathways of silver release from the sludge generated from coagulation of wastewater spiked with silver nanoparticles.

Sludge generated in wastewater treatment facilities is an integral part for the introduction of silver nanoparticles (AgNPs) to the terrestrial environment, which would cause some adverse ecosystem responses. The understanding of silver release process from the sludge is important to evaluate their risks. In this study, the amount and speciation of the released silver were investigated by taking the sludge generated by wastewater coagulation with AgNPs added (denoted as sludge) an example, and kinetic analysis and density functional theory (DFT) calculations were first used to explore the controlling steps and pathways about the silver release.

Design, synthesis, and antitumor activity evaluation of pretubulysin analogs.

Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in a variety of tumor cell lines. Although there are several total synthesis routes to tubulysin and pretubulysin reported, the commercialization still has been hampered due to the complexity of the structure. To find structurally simpler pretubulysin analogs, a series of 2-(3-(methylamino)propyl)thiazole-4-carboxamides are designed and synthesized, and their anticancer activities are screened using MCF-7 (breast cancer), and NCI-H157 (lung cancer) cell lines.

Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors.

A series of 4-aryl-5-aminoalkyl-thiazole-2-amines were designed and synthesized, and their inhibitory activity on ROCK II was screened by enzyme-linked immunosorbent assay (ELISA). The results showed that 4-aryl-5-aminomethyl-thiazole-2-amines derivatives had certain ROCK II inhibitory activities. Compound 10l showed ROCK II inhibitory activity with IC value of 20 nM.

Synthesis and Evaluation of Biological Properties of 2-Amino-thiazole-4-carboxamides: Amide Linkage Analogues of Pretubulysin.

Pretubulysin is a bio-precursor of highly toxic tetrapeptide tubulysins. Although pretubulysin has a much simpler chemical structure, it has similar anti-mitotic potency. A series of 2-amino-thiazole-4-carboxamides were designed and synthesized based on the structure of cemadotin.

The removal of silver nanoparticle by titanium tetrachloride and modified sodium alginate composite coagulants: floc properties, membrane fouling, and floc recycle.

In this study, a modified sodium alginate (MSA) composited with TiCl was used to treat the synthetic Ag nanoparticles (AgNPs) water in coagulation-ultrafiltration process. The floc properties and membrane fouling of TiCl and MSA composite coagulants (TiCl + MSA) were investigated by a laser diffraction instrument and ultrafiltration fouling model. The recycle of the AgNP-containing flocs was evaluated by XRD and photocatalytic experiments.