Growing interest in drug discovery is often advanced as drugs do not adequately increase resistance against increasing cancer cases worldwide. Molecular hybridization is a new concept in drug design and growth based on the combination of pharmacophore moieties of different bioactive substances to produce a new hybrid compound with greater affinity and efficacy, compared to the parent drugs. Say no to plagiarism. Get a tailor-made essay on "Why Violent Video Games Shouldn't Be Banned"? Get an original essayMolecular hybridization is a normal design approach of new ligands or prototypes based on the detection of pharmacophore subunits in the molecular structure of two or more well-known bioactive derivatives which, through extensive fusion of these subunits, lead to the design of new hybrid architectures that maintain pre-selected characteristics of the original models. The literature survey revealed that the history of heterocyclic chemistry begins in 1800, hand in hand with the development of organic chemistry. After World War II, there was massive explosion research in the field of heterocycles. About half of the more than six million compounds recorded in the Chemical abstract are heterocyclic. Considering the use of known model A substances, the physicochemical and pharmacological characteristics, toxicity and mechanism of action have already been evaluated. The triazole fraction is a significant and recurring insecticide, characteristic of the agrochemical structure of many biological active compounds such as cytochrome enzyme inhibitors and peptide analogue inhibitors. The class of azole antifungal agents consists of a triazole or imidazole chemical group attached to an asymmetric carbon atom as a functional pharmacophore treatment for these infections. Azole-like antifungal agents are Fluconazole, Ketoconazole, and Ptraconazole. 1, 2, 4-triazole, Voriconazole are as painkiller, antiasthmatic, anticholinergic, antibacterial. Currently, cancer has progressively become the main cause of death and will seriously jeopardize human health and existence for a long time. It has been reported that cancer can be caused by one of three ways: poor diet, genetic predisposition, and environmental contaminants. Pyrimidines and their derivatives have also been taken into consideration since the last century as they also possess diverse pharmacological properties and a wide range of biological properties. activities against unrelated DNA and RNA, diuretic, antitumor, viruses including herpes polio viruses, anti HIV, cardiovascular and so on. The characteristics possessed by 1,2,3-triazoles make them pharmaceutically significant molecules. They are stable to reduction and oxidation as well as hydrolysis under acidic and basic conditions, which indicates their high aromatic stabilization. 1,2,3-triazoles have a high dipole moment (about 5 D) and are able to actively contribute to hydrogen bond formation, as well as dipole-dipole and π-stacking interactions, which helps them bond easily with biological targets and improves their solubility. The click chemistry approach invented by Sharpless using copper(I)-catalyzed azidealkyne cycloaddition (CuAAC) led to the production of large numbers of 1,4-disubstituted 1,2,3-triazoles in very high yields. Cancer is a group of diseases in which cells grow abnormally and multiply through uncontrolled cell division. Cancer cells are metabolically more active than normal cells. It gradually invades and destroys nearby normal cells forming a nodule calledtumor. Not all tumors or nodules are benign, tumors are not cancer. It is localized and small in size that tends to grow quite slowly. It does not spread to other parts of the body and is rarely life-threatening. Both external and internal factors such as dietary fat intake, exposure to solvents and pesticides, exposure to ionizing radiation (causing leukemia, thyroid cancer, breast cancer, lung cancer and others), cigarette smoking, some viruses (HIV, HPV and hepatitis B virus) and unhealthy lifestyle (overweight, inadequate exercise, excess alcohol, insufficient quantities of fruit and vegetables, excess sugar and red meat) can cause cancer. Once DNA is affected, there are no normal control systems to prevent tumor cells from overgrowing cells and invading other tissues. Cancer is one of the most widespread and deadly diseases and a third of the world's population suffers from it. Therefore, molecules containing the triazole moiety show antitumor activities and may be able to protect drug resistance to some extent (cephatizine, antibacterial agent Tazobactum and antitumor agent7). In this review, we focus on the most relevant advances recorded in click chemistry reactions and synthesis under mild physiological conditions and with high efficiency and chemoselectivity. Literature review Chalcones and its derivatives attract more and more attention due to numerous pharmacological applications. They are the main precursors for the biosynthesis of flavonoids and exhibit various biological activities such as anti-tumor, anti-inflammatory, nitric oxide regulator and anti-hyperglycemic agents. In recent years, ionic liquids have emerged as a powerful alternative to conventional molecular organic solvents due to their particular properties, such as undetectable vapor pressure, wide liquid range, as well as ease of recovery and reuse, and that they they make a more environmentally friendly alternative to conventional molecular organic solvents. volatile organic solvents. Chalcones have a wide range of biological activity and were created to be effective as antibacterial, anti-inflammatory, antifungal, and anticancer, etc. Chalcones are overall the α,β unsaturated carbonyl compounds in which they contain the ketoethylene group. Chalcones have conjugated double bonds and a fully delocalized π electron structure on both benzene rings. Chalcone chemistry has generated intensive scientific studies worldwide. Particular interest has been focused on the synthesis and biodynamic activities of chalcones. The name “Chalcones” was given to him by Kostanecki and Tambor. These compounds are also known as benzalacetophenone or benzylidene acetophenone. In chalcones two aromatic rings are linked by a three-carbon aliphatic chain. Chalcone brings an excellent synthon so that a variety of new heterocyclics with a good pharmaceutical profile can be designed. Several methods are available for the preparation of chalcones8. Chalcones have a simple chemistry that allows for a multiplicity of substitutions with easy synthesis. Currently, a variety of methods and schemes are available for the synthesis of chalcone derivatives. In each of these methods, the most important part is the condensation of two aromatic systems (with nucleophilic and electrophilic groups) to produce the chalcone scaffold. Despite the multiplicity of substitutions allowed, we describe the reaction scheme below using the standard chalcone (1,3-diphenyl-2-propen-1-one) scaffold. Claisen-Schmidt condensation The Claisen-Schmidt condensation is one of the most common. In this reaction, chalcones are formed by condensation of benzaldehyde derivatives andof acetophenone in the presence of alkaline or acid catalysts in a liquid solvent at 50–100 °C for several hours. The conventional Claisen-Schmidt reaction is typically conducted in the liquid phase, but some reactions can occur in the solid phase (e.g., acetophenone derivatives are primarily bound to the resin and then treated with benzaldehyde derivatives) or in solvent-free phase (for example, condensation in the presence of the triazabicyclodecene catalyst). Furthermore, the use of microwaves in liquid and solvent-free Claisen-Schmidt reactions reduces synthesis times and produces good quantities of chalcones.8. Coupling reaction Chalcones are also synthesized by a coupling reaction of trabenzaldehyde and phenylacetylene in the presence of HBr and ionic liquids, such as 1-butyl-3-methyl-1H-imidazolium 4-methylbenzenesulfonate for 12 hours at 100 °C 9. Coupling reaction Carbonylative Heck coupling In the carbonylative Heck coupling reaction the chalcones are synthesized by vinyl carbonylation of the phenyl halide with styrene in the presence of carbon monoxide and using palladium (Pd) as a catalyst. One-pot synthesis One-pot synthesis is a simple but efficient environmentally friendly method that allows the synthesis of chalcones in a single reactor. This method offers numerous advantages, such as greater reaction efficiency and the elimination of the time-consuming process of purification of intermediate chemical compounds, thus saving resources and time. The reaction consists of a mixture of phenylmethanol and acetophenone in the presence of the oxidizing agent CrO3. Please note: this is just a sample. Get a custom paper from our expert writers now. Get Custom Assay In this reaction, CrO3 plays the vital role of generating benzaldehyde from phenylmethanol, which further reacts with acetophenone to produce the desired chalcone. Bioactivity of the triazole nucleus. Click chemistry of 1,2,3-triazole 45. 1,2,3-triazole is an important and well-known heterocycle in both synthetic and medicinal chemistry due to its simple synthesis via the click chemistry approach click and a wide range of biological activities. Simple copper-catalyzed 1,3-dipolar cycloadditions of substituted azides and alkynes provide regioselective 1,4-disubstituted 1,2,3-triazoles in high yields. 1,2,3-triazole with high dipole moment, remarkable stability and ability to form hydrogen bonds make it a favorable ligand of biomolecular targets. 1,2,3-triazole derivatives have been reported to exhibit various biological activities such as antidiabetic, antitubercular, anti-inflammatory, antifungal, antiviral, and antibacterial. Numerous drugs such as carboxyamidotriazole, cefatrizine, and tazobactam contain 1,2,3-triazole in their structure. Since Sharpless and colleagues published their seminal report on the so-called "click chemistry" concept, a large number of articles have been published on the use of the drug. The prototype click reaction constituted the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) to give 1,4-disubstituted 1,2,3-triazoles in very high yields under mild conditions. This metal-catalyzed reaction independently discovered in the Sharpless and MeldalClick chemistry laboratories is a modular synthetic approach towards the assembly of new molecular entities. This strategy is mainly based on the construction of carbon-heteroatom bonds using spring-loaded reagents. The broad scope of CuAAC is firmly demonstrated by use in diverse areas of life and materials sciences such as bioconjugation for drug discovery, polymer and materials science, and related areas including supramolecular chemistry. The 1,2,3-triazole core has been applied in many synthetic materials chemistry approaches 416.