BackgroundCytosolic 5′-nucleotidase 1A (NT5C1A) dephosphorylates non-cyclic nucleoside monophosphates to produce nucleosides and inorganic phosphates. Here, we investigate NT5C1A expression in pancreatic ductal adenocarcinoma (PDAC) and its impact on gemcitabine metabolism and therapeutic efficacy.

BackgroundPancreatic ductal adenocarcinoma (PDAC) is an aggressive disease with poor prognosis, and gemcitabine-based chemotherapy remains an effective option for the majority of PDAC patients. Hepatocyte nuclear factor 1α (HNF1A) is a tumor-suppressor in PDAC, but its role in gemcitabine chemo...

Chemoresistance is a major therapeutic obstacle in the treatment of human pancreatic ductal adenocarcinoma (PDAC). As an oxidative stress responsive transcription factor, nuclear factor erythroid 2-related factor 2 (Nrf2) regulates the expression of cytoprotective genes. Nrf2 not only plays a cr...

A series of hydroxamic acid derivatives of peptides related to fragments of substance P (SP) were synthesized. Methyl, ethyl or N-hydroxy-succinimide ester precursors of the desired peptides were prepared by using classical peptide synthesis methodology and these were reacted with excess hydroxy...

A few novel 1,3-dioxane carboxylic acid derivatives were designed and synthesized to aid in the characterization of PPAR α/γ dual agonists. Structural requirements for PPARα/γ dual agonism of 1,3-dioxane carboxylic acid derivatives included the structural similarity with potent glitazones in...

Early diagnosis and therapy of cancer metastasis are of great importance for disease outcome. Circulating tumor cells (CTCs) offer the ability for noninvasive tumor profiling in real time. However, simply capturing and counting tumor cells are inadequate to provide valuable information about tum...

Previous studies have reported negative findings for the association among brain monoamine oxidase B (MAO-B) and suicidal behaviour. However those studies did not adequately control their main results for the influence of confounding variables such as age at death. We have evaluated the associat...

Free radical-induced damage to lipid and protein constituents of neuronal membranes contributes to the pathophysiology of neurodegenerative diseases, including Alzheimer’s disease (AD). The development of an effective inhibitor of oxidative stress represents an important goal for the treatment ...

In the studied a series novel of lazabemide derivatives were designed, synthesized and evaluated as inhibitors of monoamine oxidase (MAO-A or MAO-B). These compounds used lazabemide as the lead compound, and the chemistry structures were modified by used the bioisostere and modification of compo...

6-(4-Isopropyl-1,4-dimethyl-4,5-dihydro-1H-imidazol-5-on-2-yl)pyridine-2-carboxylic acid (1) was used for the preparation of three copper(II) complexes, 5–7, and one cobalt(II) complex, 8. The structures of these complexes were studied in the solid phase and in solution by means of X-ray diffra...

The reactions of ethyl 2-ethoxymethylene-3-oxo-3-(polyfluoroalkyl)propionates with 3-amino-5-hydroxypyrazole result in ethyl 2,7-dihydroxy-7-(polyfluoroalkyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-carboxylates under mild conditions. These products undergo recyclization in refluxing ethanol to fo...

Acetoguanamine is an advantageous molecular precursor for a freshly identified N-H⋯O/N-H⋯N synthon, which is adequate for the design of novel multi-dimensional structures. Six compounds of acetoguanamine with various carboxylic acids pyridine-2,3-dicarboxylic acid 1, phthalic acid 2, 3,4,5-trime...

The syntheses of new terephthalic acids (8a-d) containing various polyfluoroalkyl groups (a ; CF3, b ; HCF2, c; H(CF2)3 and d ; H(CF2)5) are described in this paper. These compounds were obtained by aromatization (bromination and dehydro-bromination) of Diels-Alder adducts (2a-d and 3a-d) of pol...

Poly(arylene ether)s (9) containing pendant benzoyl groups were prepared by the aromatic substitution reaction of 2,5-difluoro-4-benzoylbenzophenone (7) with bisphenol (8) in the presence of potassium carbonate in N,N-dimethylacetamide. The polycondensation proceeded smoothly at 170°C and produ...

The structure–activity relationship of HIV-1 protease (HIV-1 PR) inhibitors containing α-hydroxy-β-amino acids is discussed. We demonstrated that substituent groups on the P1 aromatic rings of the inhibitors exert significant influence on their biological activity. Inhibitors bearing an alkyl...

Quantitative structure property relationships (QSPR) for the pKa of phenols, carboxylic acids and alcohols were developed from descriptors derived from semi-empirical molecular orbital theory quantum chemical calculations. A training set of compounds were used to refine the models and a validati...

A new synthetic route to 2,5-difluoroterephthalic acid (DFTA) was devised and from this several new series of polymers were prepared by polycondensation. This inaugural paper will cover polyesters while subsequent papers will report on keto polyethers, polyamides and other backbones derived from...

An extensive set of computed molecular properties, both steric and electronic, have been calculated using molecular orbital and empirical methods for benzoic acid (1) and a congeneric series of substituted benzoic acids, i.e. 2-, 3- and 4-fluorobenzoic acids (2–4), 2-, 3- and 4-trifluoromethyl ...

In this work, a regioselective synthesis of isocoumarins from 2-alkynylbenzoic acid is reported. The transformations proceed smoothly with good yields in water via a metal-free radical pathway. When catalytic TBAB is employed, the reaction provides various isocoumarin derivatives according to th...

Fluoroaryl containing β,β′-dioxoesters and their copper(II) chelates have been prepared by acylation of ethyl acetoacetate with 2,6-dimethoxy-3,4,5-trifluorobenzoyl, 2-methoxy-3,4,5,6-tetrafluorobenzoyl and pentafluorobenzoyl chlorides. Cyclization of these β,β′-dioxoesters leads to format...