scholarly journals Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

2021 ◽  
Vol 9 ◽  
Author(s):  
Paulina Wdowiak ◽  
Joanna Matysiak ◽  
Piotr Kuszta ◽  
Katarzyna Czarnek ◽  
Ewa Niezabitowska ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Urinary Bladder Cancer ◽  
Biological Properties ◽  
Diagnostic Methods ◽  
Major Health ◽  
Complex Disorder ◽  
Wide Range ◽  
Quinazoline Derivatives ◽  
Cyclic Compounds ◽  
Derivatives Of

Cancer diseases remain major health problems in the world despite significant developments in diagnostic methods and medications. Many of the conventional therapies, however, have limitations due to multidrug resistance or severe side effects. Bladder cancer is a complex disorder, and can be classified according to its diverse genetic backgrounds and clinical features. A very promising direction in bladder cancer treatment is targeted therapy directed at specific molecular pathways. Derivatives of quinazolines constitute a large group of chemicals with a wide range of biological properties, and many quinazoline derivatives are approved for antitumor clinical use, e.g.,: erlotinib, gefitinib, afatinib, lapatinib, and vandetanib. The character of these depends mostly on the properties of the substituents and their presence and position on one of the cyclic compounds. Today, new quinazoline-based compounds are being designed and synthesized as potential drugs of anticancer potency against bladder cancers.

scholarly journals The influence of chromone based hydrazones on lipid peroxidation and bFGF concentration in the HL-60 cell line.

2013 ◽  
Vol 60 (2) ◽  
Author(s):  
Andrzej Łazarenkow ◽  
Marta Michalska ◽  
Anna Gorąca ◽  
Marek Mirowski ◽  
Jolanta Nawrot-Modranka ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Cell Line ◽  
Significant Influence ◽  
Biological Properties ◽  
Synthetic Analogues ◽  
Wide Range ◽  
Synthetic Derivatives ◽  
Derivatives Of

Natural and synthetic derivatives of benzo-γ-pyrones (i.e. flavones, chromones, and coumarins) and their synthetic analogues possess a wide range of biological properties in vitro and in vivo. In this paper we investigated the influence of two hydrazone compounds of chromones, 3-{[(2-dimethoxytiophosphoryl)-2-methylhydrazono]-methyl}-chromen-4-one (CH-3) and 2-amino-6-chloro-3-[(2-hydroxyethyl)-hydrazonomethyl]-chromen-4-one (A-12), on lipid peroxidation and bFGF concentration in the HL-60 cells. Both of the studied compounds had a significant influence on bFGF and TBARS in ranges -137.20 ~ 380.26% and -81.66 ~ -28.68%, respectively, in comparison with the control (counted as 0%).

scholarly journals Synthesis and properties of S-derivatives of 4-amino-5-(5-methylpyrazol-3-yl)-1,2,4-triazole-3-thiol

2021 ◽  
Vol 14 (3) ◽  
pp. 268-274
Author(s):  
S. O. Fedotov ◽  
A. S. Hotsulia
Keyword(s):  
In Silico ◽  
Biological Properties ◽  
Biologically Active ◽  
Anticancer Activities ◽  
Chemical Methods ◽  
Biological Potential ◽  
In Silico Studies ◽  
Wide Range ◽  
Physical And Chemical ◽  
Derivatives Of

The combination of various heterocyclic systems with a wide range of properties is quite expedient and is, in practice, a justified direction for obtaining biologically active substances, which ultimately forms a favorable basis for the creation of drugs. In recent decades, the attention of scientists has been closely focused on nitrogen-containing heterocyclic compounds. Among such compounds, 1,2,4-triazole and pyrazole occupy a special place. Indeed, on the basis of these systems, a significant number of well-known drugs have been created, which are widely used at the present time. The aim of the work was the synthesis of S-derivatives of 4-amino-5-(5-methylpyrazol-3-yl)-1,2,4-triazole-3-thiol, study of their physical and chemical properties, pre-screening studies with subsequent establishment of the feasibility of further pharmacological studies. Materials and methods. Experimental methods of organic chemistry: synthesis using microwave activation, physical and chemical methods for the analysis of organic compounds (determination of the melting point, elemental analysis, 1H NMR, IR spectroscopy and chromatography-mass spectrometry). Methods for in silico pre-screening studies to establish the biological potential in several synthesized compounds (molecular docking). Results. 10 new S-derivatives of 4-amino-5-(5-methylpyrazol-3-yl)-1,2,4-triazole-3-thiol were synthesized. The structure of the obtained compounds was confirmed by a set of physical and chemical methods of analysis. According to the results of prescreening studies, the main directions of research of biological properties of synthesized compounds were provided. Conclusions. The expediency of using microwave irradiation in the synthesis of a series of S-alkyl derivatives of 4-amino-5-(5-methylpyrazol-3-yl)-1,2,4-triazole-3-thiol had been proved. Based on the results of in silico studies, the expediency of further studies of anti-inflammatory, antifungal and anticancer activities in several synthesized compounds had been substantiated.

Synthesis, Characterization and Antimicrobial Activity of Some Novel 1- substituted Benzimidazole Derivatives

2020 ◽  
Vol 17 (11) ◽  
pp. 1372-1379
Author(s):  
Erkut Isik ◽  
Demet Astley ◽  
Seda Yuksekdanaci ◽  
Ihsan Yasa
Keyword(s):  
Antimicrobial Activity ◽  
Experimental Studies ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Benzimidazole Derivatives ◽  
Human Immune System ◽  
Antimicrobial Drugs ◽  
Wide Range ◽  
Test Organisms ◽  
Derivatives Of

Background: Benzimidazole derivatives are an important class of heterocyclic compounds in organic chemistry as they are related to a wide range of biological properties, including antimicrobial activity. Methods: A series of 1-naphthoyl and benzoyl benzimidazole derivatives were synthesised, identified and screened for their antimicrobial activities against a number of different test organisms such as Escherichia coli, Pseudomonas aureginosa, Klebsiella pneumoniae, Staphylococcus aureus, Enterococcus faecalis, Bacillus cereus, Salmonella typhimurium, Candida albicans (yeast). Results and Discussion: Benzimidazole derivatives (3a-d) were synthesised by using 4 different aminoacids. L-methionine, L-isoleucine, D-Phenylysine and L-Phenylamine as starting materials in the study. Experimental studies involve the use of benzimidazole derivatives (3a-d) of the selected amino acids to synthesize the benzoyl and naphthoyl derivatives of benzimidazole (4a-d, 5a-c). The structures of the synthesized compounds were confirmed by spectroscopic analyses (FTIR, 1HNMR, 13C-NMR) and elemental analysis. Conclusion: In this study, only one compound (5a) showed a low MIC value against the eukaryotic microorganism C. albicans. The other six compounds showed higher antimicrobial activities against the prokaryotes C. albicans which is a normal flora in the mouth but is one of the organisms that cause infections leading to the weakening of the human immune system. Compound 5a is a candidate for future alternative antimicrobial drugs against C. albicans infections. In addition, compound 5a has a potential to be used as an inhibitor against P. aureginosa for the treatment of cystic fibrosis.

Antimicrobial Activities of Satureja khuzestanica Jamzad; A Review

2020 ◽  
Vol 20 ◽  
Author(s):  
Hossein Mahmoudvand ◽  
Behrouz Ezatpour ◽  
Leila Masoori ◽  
Abdolrazagh Marzban ◽  
Ali Moghaddam ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Biological Properties ◽  
Study Results ◽  
Wide Range ◽  
Herbal Medications ◽  
Publication Time ◽  
Satureja Khuzestanica ◽  
Medical Importance ◽  
Derivatives Of ◽  
Different Climates

: Satureja khuzestanica Jamzad. is a species native to Iran, highly important in Southwestern regions. It belongs to the Lamiaceae family and grows in different climates. A number of pharmacological properties such as analgesic, anti-inflammatory, anticancer, anti-thyroid, antioxidant, and diuretic heve been attributed to this plant. In recent years, a wide range of biological properties, extract, and essential oil of Satureja khuzestanica has been studied by researchers. In the present study, Scopus, SID, ISI, Google Scholar, and PubMed indices were used to extract research articles. No publication time constraint was considered, and the keyword “Satureja khuzestanica” was used to search articles. All extracted articles were examined by two expert researchers and those on the biologic and fundamental science properties of this plan entered the study. Results showed that S. khuzestanica has extensive research and medicinal applications. Considering the economic and medical importance of S. khuzestanica, it is hoped that more extensive studies can be conducted in future on the use of compounds and derivatives of this plant in order to obtain herbal medications to treat pathogens in human and animal.

777: Tissue Microarray Analysis of pAkt, PTEN and L-Plastin in Urinary Bladder Cancer

2005 ◽  
Vol 173 (4S) ◽  
pp. 211-211
Author(s):  
Loleta D. Harris ◽  
Tomasz Tuziak ◽  
Jorge De Lo Cerda ◽  
Anita L. Sabichi ◽  
Ying Yang ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Urinary Bladder ◽  
Tissue Microarray ◽  
Microarray Analysis ◽  
Urinary Bladder Cancer ◽  
Tissue Microarray Analysis

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

scholarly journals Knowledge, perception and screening of local dye workers regarding urinary bladder cancer in Ghana

2020 ◽  
Vol 26 (1) ◽  
Author(s):  
Babatunde M. Duduyemi ◽  
Divine Lardey Agyemang ◽  
Ernest Adankwah ◽  
Hannah Nyarko ◽  
Derrick Andoh
Keyword(s):  
Bladder Cancer ◽  
Urinary Bladder ◽  
Educational Level ◽  
Response Rate ◽  
Urinary Bladder Cancer ◽  
Clinical History ◽  
Level Of Knowledge ◽  
Knowledge Levels ◽  
Cancerous Cells ◽  
Structured Questionnaire

Abstract Background Cancer is the leading cause of death with 7.6 million deaths worldwide annually. About 19% of bladder cancer cases are attributed to environmental and occupational factors. The knowledge of any disease is very vital in the control or prevention of such disease. This study examined the knowledge and perception of urinary bladder cancer among 104 local dye workers in Ghana (Kumasi, Koforidua and Somanya). Methods A well-structured questionnaire was used to measure participants’ knowledge and perception towards bladder cancer. Forty out of the 104 participants were recruited to provide their urine samples for cytomorphological study. Thin smears were prepared and stained with Papanicolaou stain. Respondents were selected based on clinical history and working experience. Result The response rate to the questionnaires was 100% of the 104 respondents interviewed. The respondents had a mean age of 26 years. Overall, about 10% of the respondents in this study had good knowledge levels on bladder cancer and 16% had good perception of the disease. There was a significant correlation between knowledge and educational level of the participants (p < 0.001). Report of the cytomorphological study indicates that none of the samples of the participants screened had cancerous cells. Conclusion The findings suggest that level of knowledge about bladder cancer among local dye workers in this study was low, while their level of perception was just above average.

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