Studies show that arsenite induces oxidative stress and modifies cellular function via phosphorylation of proteins and inhibition of DNA repair enzymes. Autophagy, which has multiple physiological and pathological roles in cellular function, is initiated by oxidative stress and is regulated by t...

Arsenite exposure can induce a biphasic response called “hormesis”, and oxidative stress has been proposed to play critical roles in the hormesis effect. However, the precise mechanisms underlying the hormesis effect induced by arsenite is largely unknown. Recently, N6-methyladenosine (m6A) mo...

The photophysical behaviours of quinoline based red fluorescent zinc complex (QAZn) in the presence of the highly toxic AsO2− and biologically active H2PO4− ions have been explored in aqueous DMSO solution. The sequential detection of both the anions was examined using absorption and fluorescenc...

The lead hydrogen arsenite chloride precipitates (Pb2(HAsO3)Cl2) are synthesized hydrothermally due to its structure trap for lead and arsenic. The synthetic precipitates have well-developed crystalline. The crystals of lead hydrogen arsenite chloride have a series of obvious IR bands at 790, 72...

A series of 2-amino-N-benzylpyridine-3-carboxnamides, 2-amino-N-benzylpyridine-3-sulfonamides and 2-amino-3-benzylthiopyridines against c-Met were designed by means of bioisosteric replacement and docking analysis. Optimization of the 2-amino-3-benzylthiopyridine scaffold led to the identificati...

Human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated ribonuclease H (RNase H) remains an unvalidated drug target. Reported HIV RNase H inhibitors generally lack significant antiviral activity. We report herein the design, synthesis, biochemical and antiviral evaluations of a ...

The sphingomyelin synthase 2 (SMS2) is a potential target for pharmacological intervention in atherosclerosis. However, so far, few selective SMS2 inhibitors and their pharmacological activities were reported. In this study, a class of 2-benzyloxybenzamides were discovered as novel SMS2 inhibito...

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for development of various tumor types. In this study, we synthesized a series of novel 2,4-diarylaminopyrimidine derivatives possessing a unique N-(3-pyridinylmethyl)urea moiety as ALK inhibitors. The most promising anal...

Ticagrelor as a platelet aggregation antagonist can be prepared from (1R,2S)-2-(3,4-diflurophenyl)cyclopropan-1-amine that is converted from (1R,2R)-2-(3,4-diflurophenyl)cyclopropane-1-carboxylic acid ((1R,2R)-DFPCPCA)) via Curtius or Hofmann rearrangement. In this work, an efficient hydrolytic ...

The oxidation characteristic of ETBE (ethyl tert-butyl ether) was determined using ARC (accelerating rate calorimetry). Oxidation temperature and oxidation kinetics were calculated using temperature-time (T-t) and pressure-time (P-t) plots, and reaction products were analyzed by GC-MS (gas chrom...

The increasing number of weedy species resistant to dinitroaniline herbicides warrants studies on the evolutionary factors contributing to resistance evolution, including genetic inheritance of resistance traits. In this study, we investigated the genetic control of trifluralin resistance in a w...

Glucokinase (GK) is the main enzyme which controls the blood glucose levels in a safe and narrow physiological range in humans. GK activators are the novel type of therapeutic agents which act on GK enzyme and show their anti-diabetic potential. The present work was planned to synthesize and eva...

IntroductionThis trial compared the effects of lavender and bitter orange on anxiety in postmenopausal women.

A one-pot synthesis of 2,4,5-triarylated imidazoles via three-component domino reaction of 2,2-dibromo-1,2-diarylethanones, ammonium acetate, and aryl aldehydes under catalyst-free conditions is developed. The scope of this reaction is studied. A possible mechanism is proposed based on experimen...

We have developed an efficient bifunctional squaramide catalyst for the asymmetric Michael addition of ethyl α-nitroacetate to β,γ-unsaturated α-ketoesters. This organocatalytic asymmetric reaction provides convenient and valuable access to highly functionalized 2-nitro-5-oxo-3-arylhexanedio...

The five-component reaction of ethyl 2-[(2-oxopropyl)sulfanyl]acetate, aromatic aldehydes, and ammonium acetate affords two diastereomers of 5,7-diaryl-5,6,7,8-tetrahydro-1H-pyrido[3,4-b][1,4]thiazin-2(3H)-ones via a novel tandem Mannich-enamine-substitution sequence. Presumably, they are genera...

A series of 2,3-diaryl-4-thiazolidinone derivatives were synthesized and evaluated for their antiproliferative properties against two well-known cancer cell lines (A549 as human lung cancer and MDA-MB-231 as human breast cancer). Structure activity relationship (SAR) analysis resulted in the dis...

Brain metabotropic glutamate receptor 2 (mGluR2) has been proposed as a therapeutic target for the treatment of schizophrenia-like symptoms arising from increased glutamate transmission in the forebrain. However, there does not exist a reliable tool for the study of mGluR2 in human neuroimaging....

Plinabulin and KPU-300 are promising anti-microtubule agents; however, the low water solubility of these compounds (

Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40 °C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary re...