Search results for "Valuation"

Synthesis and inhibitory activity of dimethylamino-chalcone derivatives on the induction of nitric oxide synthase.

2002

A series of nine dimethylamino-chalcone derivatives (1,3-diaryl-propenones) was synthesized and screened as potential inhibitors of NO and PGE(2) production in the RAW 264.7 macrophage cell line. 4-Dimethylamino-2',5'-dimethoxychalcone (6) was found to be the most potent and dual inhibitor (IC(50s) in the submicromolar range) of NO and PGE(2) production. 2',6'-Dimethoxylation appeared to be an effective requirement for selective and potent inhibition of nitric oxide synthase induction as it was confirmed by Western blot analysis. Chalcone (6) at 25 mg kg(-1) by oral route, inhibited significantly the formation of oedema in the carrageenan-induced model of inflammation in mice.

Synthesis, biological evaluation, and: In silico studies of novel chalcone: In pyrazoline-based 1,3,5-triazines as potential anticancer agents

2020

A novel series of triazin-chalcones (7,8)a-g and triazin-N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were synthesized and evaluated for their anticancer activity against nine different cancer strains. Triazine ketones 5 and 6 were synthesized from the cyanuric chloride 1 by using stepwise nucleophilic substitution of the chlorine atom. These ketones were subsequently subjected to a Claisen-Schmidt condensation reaction with aromatic aldehydes affording chalcones (7,8)a-g. Then, N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were obtained by cyclocondensation reactions of the respective chalcones (7,8)a-g with 3,5-dichlorophenylhydrazine. Among all the evaluated compounds, chalcones 7d,g and 8g…

On the Performance of Channel Assembling and Fragmentation in Cognitive Radio Networks

2014

[EN] Flexible channel allocation may be applied to multi-channel cognitive radio networks (CRNs) through either channel assembling (CA) or channel fragmentation (CF). While CA allows one secondary user (SU) occupy multiple channels when primary users (PUs) are absent, CF provides finer granularity for channel occupancy by allocating a portion of one channel to an SU flow. In this paper, we investigate the impact of CF together with CA for SU flows by proposing a channel access strategy which activates both CF and CA and correspondingly evaluating its performance. In addition, we also consider a novel scenario where CA is enabled for PU flows. The performance evaluation is conducted based on…

ChemInform Abstract: Synthesis, Crystallographic Studies and Biological Evaluation of Some 2-Substituted 3-Indazolyl-4(3H)-quinazolinones and 3-Indaz…

2010

A multi-criteria evaluation system for arable land resource assessment

2020

This study proposed a multi-criteria evaluation system for arable land resources by combining the soil integrated fertility index (IFI) with a soil cleanliness index (based on heavy metals and metalloid content). A total of 16 typical arable land units in Chongming District, China, were evaluated using the proposed evaluation system based on 104 collected soil samples in 16 towns. The comprehensive soil evaluation scores of arable lands in 16 towns were in the range of 90.7 to 99.2 with a mean of 96.2, indicating that the arable land in all 16 towns was at the level of excellent (≥ 90.0). Lower cleanliness indices had a significant impact on the final evaluation score. In comparison with si…

Determination of major human cytochrome P450s activities in 96-well plates using liquid chromatography tandem mass spectrometry.

2007

At the early stage of drug discovery, thousands of new chemical entities (NCEs) may be screened before a single candidate can be identified for development. Evaluation of the effect of NCEs on human CYP450 enzyme activities is a key issue in pharmaceutical development as it may explain inter-subject variability, drug-drug interactions, non-linear pharmacokinetics and toxic effects. A liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method has been developed for the fast and routine analysis of major human CYP450s enzyme activities (CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4) in primary hepatocyte cell cultures. The high sensitivity and selectivity of mass …

Membrane Protein Subunit Fractionation by Means of Inverse Pore Gradient Elution Polyacrylamide Gel Electrophoresis

1996

We report here the preparative scale isolation of the four subunits of the nicotinic acetylcholine receptor (nAChR) applying short inverse pore gradient SDS gels on an elution-PAGE apparatus. The nAChR subunits are of similar molecular weights (alpha, 50.2 kDa; beta, 53.7 kDa; gamma, 56.3 kDa; delta, 57.6 kDa) and isoelectric point (approx 5.5) and share the typical properties of amphiphatic membrane proteins that are difficult to separate by chromatographic procedures. Preparative PAGE, which has proved to be the method of choice for nAChR-subunit fractionation, however, is time-consuming and achieves only moderate resolutions yielding dilute fractions. We present here the fractionation of…

Biological Evaluation of the NIR-Emissive Ruby Analogue [Cr(ddpd) 2 ][BF 4 ] 3 as a Photodynamic Therapy Photosensitizer

2018

International audience; Photodynamic therapy relies on the bioavailability of photosensitizers with suitable photophysical, chemical and biochemical properties. Although the photophysical properties, stability and high water solubility of the chromium(III) complex [Cr(ddpd)2][BF4]3 (ddpd = N,N'-dimethyl-N,N'-dipyridin-2-ylpyridine-2,6-diamine) are very favorable, its photocytotoxicity against cancerous and non-cancerous cell lines has not yet been elucidated. We now report the cytotoxicity and photocytotoxicity of the complex [Cr(ddpd)2][BF4]3 against human cervical cancer cells, human primary glioblastoma cells, human glioblastoma astrocytoma cells and non-cancerous retinal pigment epithel…

Past and Future: The Urban Landscape and the Virtuous Management of Resource Flows for a Sustainable Environment

2022

A circular process in the case of resource flows can best be expressed according to a plan that takes into account the geographical proximity and synergy between citizens and industries. The study hypothesizes the possibility of anticipating part of the recycling processes in residential urban areas. This streamlines the work phases and consumers become an active part of the process. Circular management of resource flows is an operational problem that emerges with greater severity in an urban landscape, due to the constraints generated by road networks and the need to protect basic values. It often happens that the degradation generated by the irresolute nature of the technical environmenta…

Strategies to In Vitro Assessment of Major Human CYP Enzyme Activities by Using Liquid Chromatography Tandem Mass Spectrometry

2008

At the early stage of drug discovery, thousands of new chemical entities (NCEs) may be screened before a single candidate can be identified for development. Determining the role of CYP enzymes in the metabolism of a compound and evaluating the effect of NCEs on human CYP activities are key issues in pharmaceutical development as they may explain inter-subject variability, drug-drug interactions, non-linear pharmacokinetics and toxic effects. Reliable methods for determining enzyme activities are needed to characterize an individual CYP enzyme and to obtain a tool for the evaluation of its role in drug metabolism in humans. Different liquid chromatography tandem mass spectrometry methodologi…