Rajab abuelhalawa this thesis is submitted in partial fulfillment of the requirements. It is a member of styrenes and a member of chalcones. Benzylideneacetophenone is an important member of the chalcone series. Synthesis and characterization of some novel chalcone.
This has led to the innovations of various nonlinear optical materials. In the present study, we undertook the total synthesis of several chalcones and derivatives namely chalcone, 2hydroxychalcone, 2,4. Mistry and desai120 synthesized chalcone xvi using microwave technique. They go through a variety of chemical reactions and are found beneficial in synthesis of pyrazoline, isoxazole and an assortment of heterocyclic compounds. Literature survey revealed that chalcones and pyrimidines possess a broad spectrum of biological activities like antiinflamm atory, antimalarial, antimicrobial, antidepressant, antihistamine, antitubercular and anticancer. Chalcone is a member of the class of chalcones that is acetophenone in which one of the methyl hydrogens has been replaced by a benzylidene group.
These compounds are also known as benzalacetophenone or benzylidene acetophenone. The reaction is named after two inventive researchers, r. Asian journal of biomedical and pharmaceutical sciences 2016 volume 6, issue 56. Pdf synthesis and pharmacological properties of chalcones. These are the condensation products of aromatic aldehyde with acetophenones in the presence of catalyst. Synthesis, biological evaluation, quantitativesar and. Synthesis, characterization and evaluation of antioxidant. A series of new chalcone derivatives with a general formula of. Chalcones are commonly found in plants, vegetables, and fruits. The present doctoral thesis work aims to the improvement of preexisting analytical methods as well as to the development of innovative procedures for the identification of organic dyes of artistic and archaeological interest, with special attention being devoted to sers. Literature survey reveals that chalcone derivatives possess antibacterial, antiviral, antispasmodic activities.
Not well organized, irregularly shaped, fast growing, infiltrative growth, metastatic. The mixture was kept for 24 hrs and it was acidified with 1. School of pharmaceutical sciences, rajiv gandhi proudyogiki vishwavidyalaya, airport bypass road. Hebron university faculty of graduate studies chemistry department synthesis and biological evaluation of novel adamantylated heterocyclic rings by kariman mahmoud titi supervisor. As a key enzyme of flavonoid synthesis, the synthesis of the enzyme protein of chalcone isomerase is subject to strict control. Synthesis of chalcones and derivatives appu, venothini 2010 synthesis of chalcones and derivatives. Chalcones as versatile synthons for the synthesis of 5 and 6. Well circumscribed, slow growing, non invasive, non metastatic. Interestingly, during bromination the tautomerization of the quinolin41hone ring of compounds 1ae into the correspondi.
Chemistry, ras al khaimah medical and health sciences university. Chalcone thesis chemical reactions ketone free 30day trial. Chalcone is an aromatic ketone that forms a central core for a variety of important biological compounds, which are. U poona college of pharmacy, pune, maharashtra, india 2department of pharm. Synthesis, antioxidant and antimicrobial activities of a. Chalcones are largely distributed in plants, fruits and vegetables. The chemistry of chalcones has generated intensive scientific studies throughout the world. Introduction 2 chalcones and their derivatives find application as artificial sweeteners3943, scintillator44, polymerization catalyst 4546, fluorescent whitening agent47, organic brightening agent4849, stabilizer against heat, visible light, ultraviolet light and aging. The residue was purified on column chromatography silica gel with 10% ethyl acetate in hexane to afford pure chalcones scheme 1. Natural occurring chalcones as well as synthetic chalcone analogues have demonstrated many pharmaceutical effects, including antiinflammatory, antioxidant, antiparasite, and antitumor activities. An aromatic ketone that forms the core molecule of chalcones.
The chemical profile of the compounds is as shown in table 1. Generally, chalcones are synthesised by condensation of simple or aromatic aldehydes and ketones by base catalysed or acid catalysed followed by dehydration to yield chalcones. Design, synthesis and antiproliferative activity studies of 1,2,3triazolechalcones dongjun fu, a saiyang zhang, a yingchao liu, a xiaoxin yue, b junju liu, a jian song, a ruohan zhao, a feng li, a huihui sun, a yanbing zhang a and hongmin liu a. A solventfree protocol for the green synthesis of heterocyclic chalcones sanal dev a and sunil. An elegant synthesis of 2aroylfuro3,2cquinolines 2ae from quinolonebased chalcones 1aevia bromination of the exocyclic double bond followed by furan ring formation was developed. The focus of this thesis is the investigation of the antimalarial activities of oxygenated chalcones. Masters thesis, universiti teknologi malaysia, faculty of science. The compounds with the backbone of chalcones have been reported to possess various biological activities such as antimicrobial1,2,3, antiinflammatory4, antimalarial5,6, antileishmanial7, antioxidant8, antitubercular9,10, the.
Advances in chalcones with anticancer activities volume. Pyrazolines are well known and important nitrogen containing 5membered heterocyclic compounds. Synthesis and characterization of some chalcone derivatives. Sibel demir, feyza tinmaz, necmi dege, ilhan ozer ilhan. Synthesis of biologically important striazine based chalcones. Synthesis and pharmacological properties of chalcones.
It has 1,3diaryl1ones skeletal system, which was recognized as. The scientific results here reported are the fruit of a. Synthesis and activity of a new series of chalcones as. Procedure for synthesis of chalcones of 2acetyl5methylfuran. Frederick douglass learning to read and write essay summary.
Krebecheck reported some dihydrochalcones possessing sweetening property, which is 2000 time more than that of sucrose. The middle ring is formed by the addition of a phenolic hydroxyl group to the double bond of the carbon chain connecting the two phenolic. In this study, a novel series of chalcones fatty acid esters 5be and 6be have been synthesized via the reaction of the respective chalcones with either palmitic or stearic acid. Chalcones, hetero chalcones, and bis chalcones synthetized. Generally, chalcones are obtained using an alcohol methanol3638 or ethanol 10,39,40 as the solvent. Advances in chalcones with anticancer activities bentham. Different metabolic product like flavonoids and chalcones inhibit the activity of chs in severals crops. A green method was developed for the synthesis of chalcones using glycerin as solvent.
The use of whole cyanobacteria cells in a twostep, lightcatalysed regioselective bioreduction of chalcone, leading to the formation of the corresponding dihydrochalcone, is reported. Synthesis and characterization of nonlinear optical crystals. Synthesis of chalcone derivatives royal society of chemistry. This group of compounds is widely used in anticancer research, as an antimicrobial or an antitubercular. Synthesis, characterization and biological evaluation of. Pdf synthesis and pharmacological applications of chalcones. Chalcone is converted to flavanone by chalcone isomerase fig. The rapid spread of these infections is partly facilitated by a decrease in the development of new drugs. Design and synthesis of combretastatin a4 like chalcones and. Chalcone procedure general procedure for the synthesis of. The antimicrobial activity of chalcones is being increasingly documented.
Chapter one includes information on cancer epidemiology, the history of cancer and the development of. Synthesis and characterization of organometallic chalcones functionalized with a crown ether fragment. The skeleton of these molecules is depicted in table 1 and a summary of crystallographic data is given in table 1s supplementary material s. The first two chapters are an introduction to cancer chemotherapy and the development of tubulin as a target for chemotherapy.
Scanning hall probe microscopy of magnetic vortices in very underdoped yttriumbariumcopperoxide a dissertation submitted to the department of physics and the committee on graduate studies of stanford university in partial fulfillment of the requirements for the degree of doctor of philosophy janice wynn guikema march 2004. The newly synthesized 2pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. They are precursor in biosynthesis of flavones and anthocyanin, enzymatic cyclization of 6hydroxy chalcones1,2. Chalcone thesis chemical reactions ketone free 30day. It was first isolated from chinese liquorice glycyrrhizae inflata yerra et al. Initial stages of malignant cancer may typically show benign growth.
The use of chalcones in the synthesis of medicinal. Chalcone was formed from substituted benzaldehyde archo and acetophenone arcoch. Especially interest has been focused on the synthesis and biodynamic activities of chalcones. Highly effective, regiospecific reduction of chalcone by. In computer aided instruction read download phd thesis. The first step was to synthesize 3acetyl2,5dichlorothiophene and 2acetyl5chlorothiophene as heterocyclic ketones by using friedelcrafts acylation. Dhaneshwar b 1department of pharmaceutical chemistry, b.
Aminoketone, azamichael addition, microwave irradiation, solvent free, multicomponent reaction. This thesis comprises the design and synthesis of chalcone and chromone derivatives and their use in various biological applications, particularly as anticancer. Molecular characterisation and antimicrobial activities of. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. Green synthesis and in vitro biological evaluation of. Many research groups either isolated or synthesized chalcones that possess antimicrobial activity.
Chalcones or benzylideneacetophenone are the important constituents of natural sources. Chapter one includes information on cancer epidemiology, the history of cancer. Another related class of compounds comprising 2,3disubstituted chalcones 7bd and 8bbd as well as 2amino6substitutedphenyl4substitutedphenylnicotinonitrile derivatives. A series of 102 chalcones, distinguished by their b ring substitution patterns as alkoxylated or hydroxylated members, were synthesized and evaluated for in vitro antimalarial activity against plasmodium falciparum k1. Chalcones trans 1,3diaryl2propen1ones are natural products belong to flavonoid, are considered as intermediate in the flavonoids biosynthesis, and are widespread in plants. General procedure for the synthesis of chalcones a reference. Even though the yield of the synthesis above was low, the yield was pure. Chalcones are well known intermediates for synthesizing various heterocyclic compounds. Koh 40% the chalcones are associated with different biological activities like. Synthesis of 2aroylfuro3,2cquinolines from quinolone. Chalcones chalcones are the products of the condensation of a simple or substituted aromatic moiety with a simple or substituted acetophenone in presence of base. Subsequently, the potential microbiology activity of these molecules was evaluated by testing them against the grampositive bacteria staphylococcus aureus s. Synthesis and antimicrobial activity of some chalcone.
The results of antimicrobial testing of compounds 45ac. This thesis covers work investigating the design, synthesis and evaluation of combretastatin a4 like chalcones and their analogues, and other anticancer agents. Design and synthesis of chalcone and chromone derivatives as novel anticancer agents. Design, synthesis and antiproliferative activity studies of 1. Chalcones are 1, 3diaryl2 propene 1ones belonging to favonoid family. Chalcones are used as intermediates in order to make more complex molecules. The fast developments in the field of optoelectronics and photonics have stimulated an intense search for efficient nonlinear optical nlo crystals for laser technology, optical communication, signal processing and optical data storage. Chalcones are ubiquitous in nature and they are precursors to the flavonoids family. Journal of organometallic chemistry 2017, 827, 3240.
Aug 08, 2019 in the treatment of commonly occurring diseases and biological activities these compounds possess an array. C c r h o ch oh br c c2h5 o oh br c2h5 ch3 rcho aq. This thesis describes the synthesis of a library of chalcones and several flavanones and 1,5benzothiazepines derived from chalcones and some biological studies of these compounds against neuraminidase na. Chalcones are precursor compounds for flavonoids biosynthesis in plants, and they can also be synthesized in laboratory. Metabolic products like naringenin and chalcone narigenin can inhibit chs at 100.
The increasing issues of drugresistant bacteria has quickly become a global concern as infections spread from healthcare settings to the wider community. Design and synthesis of chalcone and chromone derivatives as. This thesis includes the design and synthesis of chalcones and chromone derivatives that target mitogen activated protein kinases proteins that are involved in various processes to maintain cell viability and the tubulinmicrotubule equilibrium, which is crucial for cellular mitosis. Chalcones possess a broad spectrum of biological activities including antioxidative, antibacterial, antihelmintic, amoebicidal, antiulcer, antiviral, insecticidal, antiprotozoal, anticancer, cytotoxic and immunosuppressive. Synthesis of aminoketone by reaction of 5 amine and. Under these conditions, there is a significant decrease in the reaction time while considerable increase in the yield and purity of the products can be obtained. Narayana moorthy, sakthivel ramasamy, uma vanam, elangovan manivannan, devarajan karunagaran and piyush trivedi affiliation. They have uses in preventing coronary heart disease, and they also have antimicrobial uses. Synthesis of chalcones and the evaluation of their. All compounds showed significant antibacterial activities against both grampositive and gramnegative bacteria. Review of methods and various catalysts used for chalcone.
Synthesis and characterization of nonlinear optical. Green synthesis of chalcones and microbiological evaluation. Design and synthesis of chalcone and chromone derivatives. The name chalcones was given by kostanecki and tambor1. Investigations on the antimalarial activity of alkoxylated. They consist of openchain flavonoids in which the two aromatic rings are joined by a threecarbon. Claisenschmidt condensation is one of the most widely used methodologies for the synthesis of chalcone derivatives.
They are naturally occurring substances, are found in a number of plants and are synthetically prepared1. The synthesis and structural characterization of chalcones. Please calculate the amounts you need prior to coming to the lab so you can spend your lab time doing chemistry rather than calculations. Chalcones have close relation to flavonols, flavanones and dihydroflavonols. Promising antiinflammatory effects of chalcones via. The research work incorporated in the thesis with entitled studies on. They possess different activities like antibacterial, antifungal, antiinflammatory and anti tumor etc depending on the sub. The kinetics of chalcone formation via aldol condensation was studied using uv spectrophotometry. Pdf chalcones and their analogs have been an area of great interest in recent years. Synthesis and phase transition behaviours of new chalcone. Chemically these are 1,3diphenyl2propene1one, in which two aromatic rings are linked by a three carbon ketoethylinic system. Computer aided drug design phd thesis binge consuming in soaps dissertation. Synthesis and antimicrobial evaluation of some chalcones. Journal of chemical and pharmaceutical research, 2014, 65.
Design and synthesis of combretastatin a4 like chalcones. It is evident from literature that among the many inorganic and semi organic. Chalcones have been investigated since long due to versatile usefulness. Scribd is the worlds largest social reading and publishing site.
Schmidt, and it illustrates a method in which a benzaldehyde and acetophenone are condensed together after their treatment with each other in the presence of strong basic or acidic catalysts in a. This thesis comprises the design and synthesis of chalcone and chromone derivatives and their use in various biological applications, particularly as anticancer agents targeting proteins associated with cancer pathogenesis and as potential fluorophores for livecell imaging. Chalcone for that details introduction are as follows. Pdf chemical and structural properties of chalcones i princess. Chalcones are 1,3diphenyl2propene1one, in which two aromatic rings are linked by a three carbon. Traditionally chalcones can be synthesised by claisen schmidt condensation of acetophenone or substituted acetophenones with aldehydes. Master thesis in organic chemistry connecting repositories. Synthesis and medicinal significance of chalcones a. Synthesis of echalcones e1,3diarylprop2en1ones supplementary material in this work, which is planned for 1 session or 2 sessions 3 hours each, students individually or in groups of two will synthesize echalcone derivatives by the.
All the synthesized chalcones were active against the test microbes. These are abundant in edible plants and are considered to be precursors of flavonoids and isoflavonoids. In the present study, a series of chalcone derivatives including 17 new compounds were synthesised. The synthesis of some substituted chalcones was carried out. The structure of 3a and 3e were further confirmed by the singlecrystal xray diffraction technique. Doing the homework since dissertation guttenberg pdf download pdf. The prokaryotic microalgae cyanobacteria are known to. Glycerin was employed as a solvent in this work because it had similar properties to the cited solvents, such as polarity and organic functionality. Thesis pdf available february 2012 with 2,663 reads. H3co c cl c cl h o ch xvi naik and naik121 synthesized chalcone derivative from 2hydroxy3bromo5ethyl acetophenone. Indeed, chalcones constitute an important group of natural compounds that are especially abundant in fruits e. Chalcones are the biogenetic precursors of all known flavonoids, which play an essential role in various metabolic processes in photosynthesizing organisms.
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