scholarly journals Synthesis, Characterization and Pharmacological Screening of Some Novel 2- substituted and 1(H)-substituted Benzimidazole Derivatives as potent Anti-cancer agents

2022 ◽  
Vol 24 (1) ◽  
pp. 34-47
Author(s):  
Pankaj S. Kore ◽  
◽  
Santosh K. Singh ◽  
Shrinivas K. Mohite ◽  
◽  
...  
Keyword(s):  
Microwave Irradiation ◽  
Organic Synthesis ◽  
Structural Motif ◽  
Benzimidazole Derivatives ◽  
Chemical Transformations ◽  
Benzimidazole Ring ◽  
Biological Application ◽  
Irradiation Energy ◽  
Anti Cancer ◽  
Pharmacological Screening

The most of drugs containing Benzimidazole ring is a prominent structural motif found in numerous therapeutically active compounds. Benzimidazole and its synthetic analogues have been found to exhibit industrial, agricultural and biological application such as antitubercular, anti-inflammatory, analgesic, anticancer, anticoagulant, as well as good antifungal and anti microbial activity. Recent advances in technology considers microwave irradiation energy as the most efficient means of heating reactions for chemical transformations that can be accomplished in a minutes. Microwave irradiation assists organic synthesis (MAOS) not only helps in implementing green chemistry but also led to progress in organic synthesis. We report pharmacological screening of some novel 2 substituted and 1(h)-substituted Benzimidazole derivatives.

Eco-Friendly Synthesis of Pyrazoline Derivatives

2017 ◽  
Vol 9 (04) ◽  
Author(s):  
Mahesh G. Kharatmol ◽  
Deepali Jagdale
Keyword(s):  
Ionic Liquids ◽  
Microwave Irradiation ◽  
Organic Synthesis ◽  
Ultrasonic Irradiation ◽  
Minimal Energy ◽  
Anticancer Activities ◽  
Conventional Methods

Pyrazoline class of compounds serve as better moieties for an array of treatments, they have antibacterial, antifungal, antiinflammatory, antipyretic, diuretic, cardiovascular activities. Apart from these they also have anticancer activities. So, pertaining to its importance, many attempts are made to synthesize pyrazolines. Since conventional methods of organic synthesis are energy and time consuming. There are elaborate pathways for green and eco-friendly synthesis of pyrazoline derivatives including microwave irradiation, ultrasonic irradiation, grinding and use of ionic liquids which assures the synthesis of the same within much lesser time and by use of minimal energy

The Molecular Diversity Scope of Oxindole derivatives in Organic Synthesis.

2021 ◽  
Vol 25 ◽  
Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Fatemeh Javadi ◽  
Fatemeh Mohajer
Keyword(s):  
Organic Chemistry ◽  
Organic Synthesis ◽  
Molecular Diversity ◽  
Biological Properties ◽  
Organic Reactions ◽  
Microbial Properties ◽  
Anti Cancer

: The role of oxindole derivatives is discussed as starting materials in diverse organic reactions including two and more components between the years 2014 until 2020. Oxindoles are famous because of their biological properties for instance chromanone-fused polycyclic pyrrolidinyl-dispirooxindoles, functionalized polycyclic spiro-fused carbocyclicoxindole, and 3,3-disubstituted oxindoles have anti-cancer, anti-tumor, and anti-microbial properties, respectively. Therefore, various methods for synthesizing the oxindole structures have received more attention in organic chemistry.

Sēra dioksīda fizikāli ķīmisko īpašību pielietojums jaunu organiskās sintēzes metožu izstrādē / Development of New Organic Synthesis Methods Based on Physico-Chemical Properties of Sulfur Dioxide

2021 ◽  
Author(s):  
◽  
Krista Gulbe
Keyword(s):  
Organic Synthesis ◽  
Chemical Properties ◽  
Coupling Reaction ◽  
Synthetic Methods ◽  
Synthesis Methods ◽  
Chemical Transformations ◽  
Scientific Publications ◽  
Cross Coupling Reaction ◽  
Aryl Acetylenes ◽  
The Republic

The Doctoral Thesis has been prepared as a collection of thematically related scientific publications comprising five publications in the SCI journals, one patent of the Republic of Latvia, and one application for patent of the Republic of Latvia. We have carried out fundamental research on the applications of SO2 as a solvent and reagent in organic synthesis. We have developed several novel synthetic methods that represent the use of liquid SO2 as a solvent for chemical transformations that proceed via carbenium ion intermediates: a) hydration of aryl acetylenes; b) hydrohalogenation of aryl acetylenes; c) ring opening of methylenecyclopropanes with halides; d) glycosylation with glycosyl fluorides. By employing DABSO as an SO2 surrogate, we have also discovered the catalytic activity of Ru(II) complexes towards sulfonylative cross coupling reaction. This finding has been applied for the synthesis of sulfonyl derived compounds.

Microwaves in organic synthesis: Synthesis of pyridazinones, phthalazinones and pyridopyridazinones from 2-oxo-arylhydrazones under microwave irradiation

2006 ◽  
Vol 43 (6) ◽  
pp. 1575-1581 ◽  
Author(s):  
Balkis Al-Saleh ◽  
Morsy Ahmed El-Apasery ◽  
Noha M. Hilmy ◽  
Mohamed H. Elnagdi
Keyword(s):  
Microwave Irradiation ◽  
Organic Synthesis

Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent, and Evaluation for CDK2 Inhibition Activity

2021 ◽  
Vol 17 ◽  
Author(s):  
Rania Helmy Abd El-Hameed ◽  
Samar Said Fatahala ◽  
Amira Ibrahim Sayed
Keyword(s):  
Cell Lines ◽  
Docking Study ◽  
Binding Pocket ◽  
Kinase Assay ◽  
Benzimidazole Derivatives ◽  
Pharmacological Activities ◽  
Anticancer Compounds ◽  
Anti Cancer ◽  
Hct 116

Background: Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules, they can easily interact with biomolecules of living systems. Objective: A series of substituted 2-thiobezimidazoles has been synthesized .Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell-lines. Methods: The spectral data of the synthesized compounds were characterized. Docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib were performed. Results: Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in CDK-ATP binding pocket. 3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib. Conclusion: Against all tested compounds ; two compounds 3c &3l were found active against two types of cell-lines.

Transformation "Insulator-Conductor" after Laser Irradiation of the Polymer Films

2011 ◽  
Vol 496 ◽  
pp. 50-54
Author(s):  
Jimsher N. Aneli ◽  
Elena F. Semiletova ◽  
Nana V. Bakradze ◽  
Teimuraz N. Dumbadze
Keyword(s):  
Laser Irradiation ◽  
Phenol Formaldehyde ◽  
High Vacuum ◽  
Polymer Materials ◽  
Chemical Transformations ◽  
Chemical Structures ◽  
Irradiation Energy ◽  
Electrical Conducting ◽  
Physical And Chemical ◽  
Paramagnetic Properties

Abstract: Formation of electrical conducting channels with paramagnetic properties on the surface of three type polymer plates (phenol-formaldehyde and epoxy resins, polyacrylonitrile) under influence of CO2 laser irradiation at the presence of air have been studied. It is shown that the magnitude of surface resistance of the investigated polymers depends on polymer type and irradiation energy. The appearance of electrical conducting regions in the polymer materials is due to laser-chemical transformations of macromolecular physical and chemical structures near the polymer plate surfaces, leading to formation of double conjugated bonds. These structures are characterized also with paramagnetic properties- by method of ESR the free radicals are discovered in the transformed regions of polymers. The obtained results practically are analogous to ones obtained in such polymers after thermal treatment at high temperatures. However there are some advantages: in the latter case for obtaining of conducting materials on the base of dielectric polymers it is necessary to use a high vacuum. Besides of such method does not allow the formation of conducting channels with desired square and configuration on the surface of polymer plates in very short time (about several seconds) at present of air.

Microwave irradiation in organic synthesis

2005 ◽  
Vol 74 (11) ◽  
pp. 969-1013 ◽  
Author(s):  
Nelly N Romanova ◽  
Alexander G Gravis ◽  
Nikolai V Zyk
Keyword(s):  
Microwave Irradiation ◽  
Organic Synthesis

Ethenesulfonyl Fluoride (ESF) and Its Derivatives in SuFEx Click Chemistry and More

Synthesis ◽  
2019 ◽  
Vol 52 (05) ◽  
pp. 673-687 ◽  
Author(s):  
Yan-Ping Meng ◽  
Shi-Meng Wang ◽  
Wan-Yin Fang ◽  
Zhi-Zhong Xie ◽  
Jing Leng ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Click Chemistry ◽  
Exchange Reaction ◽  
Organic Synthesis ◽  
Medicinal Chemistry ◽  
Materials Science ◽  
Click Reaction ◽  
Chemical Properties ◽  
Chemical Transformations ◽  
Absolute Reliability

The sulfur(VI) fluoride exchange reaction (SuFEx), developed by Sharpless and co-workers in 2014, is a new category of click reaction that creates molecular connections with absolute reliability and unprecedented efficiency through a sulfur(VI) hub. Ethenesulfonyl fluoride (ESF), as one of the most important sulfur(VI) hubs, exhibits extraordinary reactivity in SuFEx click chemistry and organic synthesis. This review summarizes the chemical properties and applications of ESF in click chemistry, organic chemistry, materials science, medicinal chemistry and in many other fields related to organic synthesis.1 Introduction2 Chemical Transformations of ESF3 Chemical Transformations of 2-Arylethenesulfonyl Fluorides4 Novel SuFEx Reagents Derived from ESF5 Applications of ESF Derivatives in Medicinal Chemistry6 Applications of ESF Derivatives in Materials Science7 Conclusion

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