In the present study, a series of new substituted N-11-(4′-N-aryl carboxamido/N-(aryl)-α-phenyl-acetamido-piperazinyl)-dibenz[b,f][1,4]-oxazepine derivatives were designed on a revised structural model, length and nature of linker and introduced aryl group. All the compounds (MJ1–MJ12) were s...
A novel series of phenylimino-10H-anthracen-9-ones and 9-(phenylhydrazone)-9,10-anthracenediones were synthesized and evaluated for interaction with tubulin and for cytotoxicity against a panel of human tumor cell lines. The 10-(3-hydroxy-4-methoxy-phenylimino)-10H-anthracen-9-one 15h and its di...
Echinoderm microtubule-associated protein-like 4 (EML4)–anaplastic lymphoma kinase (ALK) is a valid therapeutic target for the treatment of EML4–ALK-positive non-small cell lung cancer (NSCLC). We discovered 12c as a novel and potent EML4–ALK inhibitor through structural optimization of 5a. I...
The synthesis of substituted benzaldehydes, benzoic acids, heterocyclic aromatic aldehydes and acids has been studied via the oxidation of the aromatic alcohols with air under mild pressure (
1.1. The major glutathione S-transferase (GST) from the common squid Loligo vulgaris has been purified and shown to be a homodimer of subunit molecular mass 24,000 and pI 6.8.2.2. It has high activity towards 1-chloro-2,4-dinitrobenzene, p-nitrobenzyl chloride, 4-hydroxynon-2-enal and linoleic a...
Representing a multifunctional complex group of proteins, glutathione S- transferases (GSTs) play a major role in the phase II detoxification process in a wide range of organisms. This study focused on the potential detoxification ability of disk abalone (Haliotis discus discus) GST theta (AbGST...
Glutathione S-transferases (GSTs) are essential drug-metabolizing enzymes, involved in conjugation of various endogenous and exogenous substrates. Cynomolgus macaque is an important primate species in drug metabolism studies; however, cynomolgus GSTs have not been fully characterized. In this st...
The preparation of both enantiomers of 1-(2-amino-3-nitrophenoxy)-3-(tert-butylamino)-2-propanol from the enantiomeric glycidyl tosylates is described.
The new antifungal strobilurins I (1) and K (19) are 3,4-dihydro-2H-benzo[b][1,4]dioxepin derivatives. Their structure and stereochemistry was determined by degradation to aldehyde 3. Both enantiomers of 3 were synthesised and the absolute configurations assigned by the high-field 1H NMR variant...
The decline in amphibian populations is a critical threat to global biodiversity, and pesticide pollution is considered as one of the major factors. Although effects of single pesticides on amphibians have been documented, toxicological interactions prevailing in mixtures of pesticides have not ...
Rice sheath blight, a major rice disease caused by Rhizoctonia solani, has become an increasingly serious problem in modern rice production systems. Managing this disease is a challenge, and chemical control with fungicides is currently the most effective and reliable method. Here, the combined ...
Fungicide application is considered a valid management strategy for fusarium head blight (FHB) in wheat and deoxynivalenol (DON) accumulation in grain. Its efficacy, however, varies greatly depending on the severity of the epidemic, cultivar resistance, fungicide type, timing of fungicide applic...
This research was conducted in Southern Italy over two growing seasons to evaluate the effect of strobilurin application on the ethylene production of flowers (EF) and on the yield and quality parameters of processing tomato grown under moderate water deficit conditions. The following two irriga...
Strobilurins have been reported highly toxic to non-target aquatic organisms but few illustrated how they cause toxic effects on algae. This study investigated the acute toxicity of Kresoxim-methy (KRE), Pyraclostrobin (PYR), Trifloxystrobin (TRI) and Picoxystrobin (PIC) on two algae and their t...
Tail-anchored membrane proteins (TAMPs) are relatively simple membrane proteins characterized by a single transmembrane domain (TMD) at their C-terminus. Consequently, the hydrophobic TMD, which acts as a subcellular targeting signal, emerges from the ribosome only after termination of translati...
Weanling rats fed a diet containing tellurium develop a peripheral neuropathy characterized by a highly synchronous primary demyelination; this demyelination is followed closely by a period of rapid remyelination. The demyelination is related to the inhibition of squalene epoxidase activity, whi...
Receptors assembled from the products of a neuronal β4α3α5 NAChR gene cluster depend on these genes being coordinately regulated in particular populations of neurons. Little is known, however, about the transcriptional mechanisms that are likely to underlie their co-expression in correct neur...
We have isolated cDNA clones encoding SCIP, a POU domain gene expressed by myelin-forming glia of the central and peripheral nervous systems. In purified Schwann cells cultured in the absence of neurons, expression of SCIP is suppressed. This suppression is relieved by cAMP, and induction of SCI...
BackgroundCognitive and psychosocial impairment has been associated with increased levels of C-reactive protein (CRP) and homocysteine in bipolar disorder, but gender differences have seldom been studied.
SCIP is a POU domain transcription factor expressed by Schwann cells, the myelin-forming glial cells of the peripheral nervous system. In this study, we investigate SCIP regulation of gene encoding P0, the major structural protein of peripheral myelin. We find that SCIP represses transcription o...
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