scholarly journals Optimized Synthesis of New N-Mustards Based on 2-Mercaptobenzoxazole Derivatives with Antitumor Activity

Biomedicines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 476
Author(s):  
Corina Cheptea ◽  
Valeriu Sunel ◽  
Ana Cezarina Morosanu ◽  
Dan Gheorghe Dimitriu ◽  
Mihaela Maria Dulcescu-Oprea ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Side Chain ◽  
Stable Configuration ◽  
Quantum Chemical Analysis ◽  
Chemical Structures ◽  
Physico Chemical ◽  
Ehrlich Ascites ◽  
Mixed Anhydrides ◽  
Cytotoxic Group ◽  
Made In

New di-(β-chloroethyl)-amides of some acids derived from 2-mercaptobenzoxazole were prepared by reaction of the corresponding pivalic mixed anhydrides with di-(β-chloroethyl)-amine. A study regarding the optimization of the chemical reactions was made for the case of di-(β-chloroethyl)-amines. The quantum chemical analysis by Spartan’14 was made in order to establish the most stable configuration of the ground electronic states for the obtained chemical structures and some physico-chemical parameters of N-mustards reported in this paper. Mercaptobenzoxazoles substituted in the side chain with the cytotoxic group show antitumor activity and they inhibit Ehrlich Ascites in an appreciable proportion compared to the drug I.O.B.-82, as our studies evidenced.

SCAM analysis reveals a discrete region of the pore turret that modulates slow inactivation in Kv1.5

2007 ◽  
Vol 292 (3) ◽  
pp. C1041-C1052 ◽  
Author(s):  
Cyrus Eduljee ◽  
Thomas W. Claydon ◽  
Vijay Viswanathan ◽  
David Fedida ◽  
Steven J. Kehl
Keyword(s):  
Potassium Concentration ◽  
Chemical Properties ◽  
Current Amplitude ◽  
Side Chain ◽  
Slow Inactivation ◽  
Substituted Cysteine Accessibility ◽  
Physico Chemical ◽  
External Potassium ◽  
Positively Charged ◽  
Made In

In Kv1.5, protonation of histidine 463 in the S5-P linker (turret) increases the rate of depolarization-induced inactivation and decreases the peak current amplitude. In this study, we examined how amino acid substitutions that altered the physico-chemical properties of the side chain at position 463 affected slow inactivation and then used the substituted cysteine accessibility method (SCAM) to probe the turret region (E456-P468) to determine whether residue 463 was unique in its ability to modulate the macroscopic current. Substitutions at position 463 of small, neutral (H463G and H463A) or large, charged (H463R, H463K, and H463E) side groups accelerated inactivation and induced a dependency of the current amplitude on the external potassium concentration. When cysteine substitutions were made in the distal turret (T462C-P468C), modification with either the positively charged [2-(trimethylammonium)ethyl] methanethiosulfonate bromide (MTSET) or negatively charged sodium (2-sulfonatoethyl) methanethiosulfonate reagent irreversibly inhibited current. This inhibition could be antagonized either by the R487V mutation (homologous to T449V in Shaker) or by raising the external potassium concentration, suggesting that current inhibition by MTS reagents resulted from an enhancement of inactivation. These results imply that protonation of residue 463 does not modulate inactivation solely by an electrostatic interaction with residues near the pore mouth, as proposed by others, and that residue 463 is part of a group of residues within the Kv1.5 turret that can modulate P/C-type inactivation.

scholarly journals Optimal Solutions for the Use of Sewage Sludge on Agricultural Lands

Water ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 585
Author(s):  
Catalina Iticescu ◽  
Puiu-Lucian Georgescu ◽  
Maxim Arseni ◽  
Adrian Rosu ◽  
Mihaela Timofti ◽  
...  
Keyword(s):  
Heavy Metals ◽  
Sewage Sludge ◽  
Agricultural Production ◽  
Agricultural Land ◽  
Chemical Characteristics ◽  
Optimal Solutions ◽  
Physico Chemical ◽  
Agricultural Areas ◽  
The Impact ◽  
Made In

The use of sewage sludge in agriculture decreases the pressure on landfills. In Romania, massive investments have been made in wastewater treatment stations, which have resulted in the accumulation of important quantities of sewage sludge. The presence of these sewage sludges coincides with large areas of degraded agricultural land. The aim of the present article is to identify the best technological combinations meant to solve these problems simultaneously. Adapting the quality and parameters of the sludge to the specificity of the land solves the possible compatibility problems, thus reducing the impact on the environment. The physico-chemical characteristics of the fermented sludge were monitored and optimal solutions for their treatment were suggested so as to allow that the sludge could be used in agriculture according to the characteristics of the soils. The content of heavy metals in the sewage sludge was closely monitored because the use of sewage sludge as a fertilizer does not allow for any increases in the concentrations of these in soils. The article identifies those agricultural areas which are suitable for the use of sludge, as well as ways of correcting some parameters (e.g., pH), which allow the improvement of soil quality and obtained higher agricultural production.

Cholinium-amino acid based ionic liquids: a new method of synthesis and physico-chemical characterization

2015 ◽  
Vol 17 (32) ◽  
pp. 20687-20698 ◽  
Author(s):  
Serena De Santis ◽  
Giancarlo Masci ◽  
Francesco Casciotta ◽  
Ruggero Caminiti ◽  
Eleonora Scarpellini ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Amino Acid ◽  
Room Temperature ◽  
Chemical Characterization ◽  
New Method ◽  
Room Temperature Ionic Liquids ◽  
Synthetic Method ◽  
Chemical Structures ◽  
Physico Chemical ◽  
Wide Range

Fourteen cholinium-amino acid based room temperature ionic liquids were prepared using a cleaner synthetic method. Chemicophysical properties were well correlated with the wide range of amino acid chemical structures.

Topological characterization of dendrimer, benzenoid, and nanocone

2018 ◽  
Vol 74 (1-2) ◽  
pp. 35-43
Author(s):  
Wei Gao ◽  
Muhammad Kamran Siddiqui ◽  
Najma Abdul Rehman ◽  
Mehwish Hussain Muhammad
Keyword(s):  
Chemical Properties ◽  
Chemical Compounds ◽  
Topological Indices ◽  
Zagreb Index ◽  
Topological Characterization ◽  
Complex Molecules ◽  
Chemical Structures ◽  
Physico Chemical ◽  
Quantitative Structure Activity Relationships

Abstract Dendrimers are large and complex molecules with very well defined chemical structures. More importantly, dendrimers are highly branched organic macromolecules with successive layers or generations of branch units surrounding a central core. Topological indices are numbers associated with molecular graphs for the purpose of allowing quantitative structure-activity relationships. These topological indices correlate certain physico-chemical properties such as the boiling point, stability, strain energy, and others, of chemical compounds. In this article, we determine hyper-Zagreb index, first multiple Zagreb index, second multiple Zagreb index, and Zagreb polynomials for hetrofunctional dendrimers, triangular benzenoids, and nanocones.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

scholarly journals Antitumor potential of Citrus limetta fruit peel in Ehrlich ascites carcinoma bearing Swiss albino mice

2012 ◽  
Vol 2 (1) ◽  
pp. 10 ◽  
Author(s):  
Sriparna Kundusen ◽  
Asis Bala ◽  
Biswakanth Kar ◽  
Sanjib Bhattacharya ◽  
Upal K. Mazumder ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Cell ◽  
Life Span ◽  
Blood Cells ◽  
Tumor Volume ◽  
Ehrlich Ascites Carcinoma ◽  
Viable Tumor Cell ◽  
Fruit Peel ◽  
Ehrlich Ascites ◽  
Citrus Limetta

<em>Citrus limetta </em>Risso (Rutaceae), commonly known as sweet lime in English and <em>Mousambi</em> in India, has been traditionally used for several medicinal purposes. This study explored the relationship between <em>Citrus limetta </em>fruit peel and its antitumor activity against Ehrlich ascites carcinoma (EAC) bearing mice. The antitumor activity of methanol extract of peel of <em>Citrus limetta</em> fruits (MECL) was evaluated against EAC cell line in Swiss albino mice. Twenty-four hours after intraperitoneal inoculation of tumor EAC cells in mice, MECL was administered at 200 and 400 mg/kg body weight i.p. daily for nine consecutive days. On the 10th day, half of the mice were sacrificed for the estimation of tumor growth (tumor volume, viable and non-viable tumor cell counts), and hematologic parameters (red blood cells, white blood cells and hemoglobin). The rest were kept alive for assessment of survival parameters, <em>i.e. </em>median survival time and percentage increase in life span of EAC bearing mice. Intraperitoneal administration of MECL at the doses of 200 and 400 mg/kg for nine days to the carcinoma induced mice demonstrated a significant (P&lt;0.001) decrease in tumor volume, viable tumor cell count, tumor weight and a significant (P&lt;0.001) improvement in hematological parameters and life span as compared to the EAC control mice. The present study establishes marked and dose dependant anti-tumor effect of <em>C. limetta </em>fruit peel against Ehrlich ascites carcinoma bearing Swiss mice.

ANTITUMOR ACTIVITY OF CAPPARIS SEPIARIA ON EHRLICH ASCITES CARCINOMA IN MICE

2011 ◽  
Vol 2 (4) ◽  
Author(s):  
Y VenuGopal ◽  
Ravindranath A ◽  
Kalpana G ◽  
Prabhaker Reddy.V
Keyword(s):  
Antitumor Activity ◽  
Ehrlich Ascites Carcinoma ◽  
Ehrlich Ascites
Sign in / Sign up

Export Citation Format

Share Document