Biguanides, such as the diabetes therapeutics metformin and phenformin, have shown antitumor activity both in vitro and in vivo. However, their potential effects on the tumor microenvironment are largely unknown. Here we report that phenformin selectively inhibits granulocytic myeloid-derived su...

Inactivation of the tumor suppressor neurofibromin 1 (NF1) presents a newly characterized melanoma subtype, for which currently no targeted therapies are clinically available. Preclinical studies suggest that extracellular signal-regulated kinase (ERK) inhibitors are likely to provide benefit, a...

SummaryAMPK acts downstream of the tumor suppressor LKB1, yet its role in cancer has been controversial. AMPK is activated by biguanides, such as metformin and phenformin, and metformin use in diabetics has been associated with reduced cancer risk. However, whether this is mediated by cell-auton...

Two hypercrosslinked polymeric adsorbents NG-99 and NG-100 were employed to remove four phenylhydrazine derivatives, phenylhydrazine (PH), 1-methyl-1-phenylhydrazine (1-MPH), 1-acetyl-2-phenylhydrazine (1-APH) and p-methylphenylhydrazine (p-MPH) from aqueous solutions. A comparison of the thermo...

The Schiff base analogue (E)-2-(1-(2-phenyl hydrazono)ethyl)naphtholen-1-ol was synthesized by condensation reaction of 2-acetyl-1-hydroxynaphthol and phenylhydrazine hydrochloride in the presence of sodium acetate in ethyl alcohol under reflux conditions. The product obtained was characterized ...

Free radical production from the reaction of hydrazine and 1-acetyl-2-phenylhydrazine (AcPhHZ) with oxyhaemoglobin and with human red blood cells, has been observed by the electron spin resonance technique of spin trapping. Using the spin trap 5,5-dimethyl-1-pyrroline-N-oxide (DMPO), the free ra...

The reactions of 1-acetyl-2-phenylhydrazine, an accelerator used in anaerobic adhesives, were studied in the presence of transition metal ions and typical cure components. The reaction compounds have been identified and a novel cure mechanism is proposed.

ObjectiveAnticholinesterase drugs may produce paradoxical neuromuscular block when administered at shallow levels of neuromuscular block. The objective of this study was to evaluate the effects of neostigmine and edrophonium when administered at near-complete reversal from nondepolarizing block ...

ObjectiveTo examine the effects of neostigmine, an acetylcholinesterase inhibitor that has been used to treat impaired bladder emptying on diabetic rat urinary bladder smooth muscle.

SummaryNeostigmine bromide used for the treatment of functional megacolon in very low dosage nevertheless led to severe and prolonged poisoning. The role functional megacolon may have played in this is discussed.

Study ObjectiveThe aim of this study is to compare the hemodynamic effects of neostigmine-atropine combination and sugammadex in patients with cardiac problems undergoing noncardiac surgery.

During surgery, changes in intraocular pressure (IOP) can be observed resulting from several factors, such as airway manipulations and drugs used. We aimed to investigate the effects of sugammadex and neostigmine on IOP, hemodynamic parameters, and complications after extubation. Our study compr...

Neostigmine is a carbamate inhibitor of acetylcholinesterase, the enzyme responsible for hydrolyzing acetylcholine at synapses to terminate cholinergic signaling. It is mainly used postoperatively under the brand name “Bloxiverz” to reverse shallow levels of neuromuscular blockade induced by n...

A novel, simple, rapid, selective and sensitive method for the determination of neostigmine (Ns) ion in its bulk powder, different pharmaceutical dosage forms, and biological fluids (plasma and urine) using four modified carbon paste electrodes was developed. Sensor 1 is based on ion-association...

A series of novel N,N′′-diaryl cyanoguanidines were synthesized by reacting diphenyl N-cyanocarbonimidate with sulfanilamide followed by treatment of the obtained cyano-O-phenylisourea with substituted aromatic amines. The newly prepared N,N′′-diaryl cyanoguanidines showed a very interesting...

A series of unsymmetrically disubstituted urea derivatives 1–28 has been synthesized and screened for their antiglycation activity in vitro. Compounds 26 (IC50 = 4.26 ± 0.25 μM), 1 (IC50 = 5.8 ± 0.08 μM), 22 (IC50 = 4.26 ± 0.25 μM), 6 (IC50 = 6.4 ± 0.02 μM), 5 (IC50 = 6.6 ± 0.26 μM), ...

p38α mitogen activated protein kinase (MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders. A series of fifteen pyrazolyl urea derivatives (3ao) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant potential. Compounds 3ae, 3g and 3h s...

Combretastatin A-4 (CA-4) is a well-studied and attractive molecular template to develop new antimitotics. Several thousand of modifications were performed on the ring B and the ethenyl bridge of CA-4 but only a few involved the trimethoxyphenyl moiety (TMP, ring A) often considered essential to...

EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing subst...

Herein we report for the first time an efficient synthetic procedure for the preparation of N-aryl-N’-ureido-O-sulfamates (AUSs) as a new class of Carbonic Anhydrase Inhibitors (CAIs). The compounds were tested for the inhibition of several human (h) Carbonic Anhydrase (CA; EC 4.2.1.1) isoforms...