Search results for "DERIVATIVES"

3-(6-Phenylimidazo [2,1-

2019

A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increa…

Xanthones and sesquiterpene derivatives from a marine-derived fungus Scopulariopsis sp.

2016

Abstract Two new xanthone derivatives, 12-dimethoxypinselin ( 1 ) and 12- O -acetyl-AGI-B4 ( 2 ), as well as two new phenolic bisabolane-type sesquiterpenes, 11,12-dihydroxysydonic acid ( 15 ) and 1-hydroxyboivinianic acid ( 16 ), together with one new alkaloid, scopulamide ( 21 ) and one new α-pyrone derivative, scopupyrone ( 26 ), in addition to twenty-three known compounds ( 3 – 14 , 17 – 20 , 22 – 25 , 27 – 29 ) were isolated from solid rice cultures of the marine-derived fungus Scopulariopsis sp. obtained from the Red Sea hard coral Stylophora sp. All compounds were unambiguously identified through extensive NMR spectroscopic analyses, and by comparison with the literature. Marfey's re…

ChemInform Abstract: Non-Steroidal Antiinflammatory Agents. Part 23. Synthesis and Pharmacological Activity of Enaminones which Inhibit Both Bovine C…

2010

Modeling of the viscoelastic behavior of paving bitumen using fractional derivatives

2009

The paving grade bitumen used in the production of asphalt mixtures for road construction is significantly able to affect the in-service performances of flexible road pavements. It has been proved that, when subjected to loading conditions comparable with most pavement operating conditions, bituminous binders behave as linear visco-elastic materials. The aim of this paper is to propose a model based on fractional differential equations which is able to describe the behavior of bituminous binders in the linear viscoelastic range. Shear creep testing and creep recovery testing were carried out over a range of temperatures and by applying a stress level which makes it possible to maintain the …

Pharmacokinetics and pharmacodynamics of hydroxyethyl starch in hypovolemic pigs; a comparison of peripheral and intraosseous infusion.

1999

Intraosseous (i.o.) infusion is considered a useful technique for the administration of medications and fluids in emergency situations when peripheral intravascular access is not possible. This study investigated the effectiveness of i.o. versus intravenous (i.v.) infusion of hydroxyethyl starch (HES 200/0.5) in hypovolemic pigs. Twenty-three pigs (8- to 9-week-old) were anaesthesized, instrumented and blood was withdrawn (25-30 ml/kg) to50 mmHg mean arterial pressure (MAP). The animals were left untreated in haemorrhage for 30 min. Relevant haemodynamic parameters were monitored and blood samples were collected for blood gas and HES concentration analysis. Infusion of HES via i.v. or i.o. …

Cyclotriveratrylene-Containing Porphyrins

2016

International audience; The C-3-symmetric cyclotriveratrylene (CTV) was covalently bonded via click chemistry to 1, 2, 3, and 6 zinc(II) porphyrin units to various host for C-60. The binding constants, Ka, were measured from the quenching of the porphyrin fluorescence by C-60. These constants vary between 400 and 4000 M-1 and are considered weak. Computer modeling demonstrated that the zinc(II) porphyrin units, [Zn], exhibit a strong tendency to occupy the CTV cavity, hence blocking the access for C-60 to land on this site. Instead, the pincer of the type [Zn]-[Zn] and in one case [Zn]-CTV, were found to be the most probable geometry to promote host-guest associations in these systems.

Comparative investigations of hydroxyamine carane derivative and its R,S-diastereoisomers with strong local anesthetic activity

2001

Our previously conducted pharmacological screening led as to the discovery of the strong local anesthetic activity of the compound designated as KP-23. Earlier crystallographic studies revealed that the compound KP-23 crystallized in diastereoisomeric form in lowest symmetry. The aim of these comparative investigations was to evaluate anesthetic activity of KP-23 and its R,S-diastereoisomers, which were synthesized at the Institute of Organic Chemistry, Biochemistry and Biotechnology, Wroclaw University of Technology.

ChemInform Abstract: Oxidative (Cross-)Coupling Reactions Mediated by C-H Activation of Thiophene Derivatives by Using Molybdenum(V) Reagents.

2015

The use of MoCl5 renders possible the preparation of various synthetically important polycyclic thienoacenes.

ChemInform Abstract: New Porphycene Ligands: Octaethyl- and Etioporphycene (OEPc and EtioPc) - Tetra- and Pentacoordinated Zinc Complexes of OEPc.

2010

Synthesis of fluorinated amino acid derivatives through late-stage deoxyfluorinations

2018

Abstract Fluorine chemistry has represented a hot topic in drug research over the last decade. Because of their pharmaceutical potential, fluorine-containing amino acids and related derivatives have acquired high importance among medicinal chemists. Therefore their synthesis and the development of various synthetic methods for these types of molecular scaffolds have gained increasing interest in synthetic organic chemistry. The current review focuses on synthetic protocols towards fluorine-containing amino acid derivatives through late-stage fluorination with various nucleophilic reagents, describing the access of various open-chain and cyclic α-, β-, γ-amino acid derivatives.