: The [4+2] Diels-Alder cycloaddition has been widely used for the synthesis of six-member scaffolds. In recent years, there have been significant developments in this area, including the discovery and design of novel dienes and dienophiles with improved reactivity and selectivity. These new building blocks can be used to develop diverse molecular structures with functional group compatibility. Additionally, there is the use of catalytic systems and metal-mediated reactions to enable asymmetric [4+2] cycloadditions, resulting in enantiomerically enriched products. Overall, recent studies related to [4+2] Diels-Alder cycloaddition using numerous dienes, dienophiles, and catalysts in different reaction conditions have significantly improved the efficiency, selectivity, and versatility of the reaction, making it an increasingly important tool in the synthesis of complex organic molecules as presented in this review. These advancements offer exciting possibilities for the development of new methods and reagents for the construction of six-membered rings and the synthesis of bioactive compounds.

Recently released Globocan-2020 report has been disclosed an increase in new cancer cases, cancer deaths, and 5-year prevalence cases worldwide. The higher percent proportions of cancer deaths as compared to their incidence percentage in Asia and Africa. Cancer is a genetic but not inheritable disease that consists of various abnormal cells. Depending upon the nature and site of availability of cells cancer can spread all over the body. These abnormal cells can grow infinitely in which tyrosine kinases (TKs) play an important role as mediators for cellular signal transduction processes during migration, metabolism, proliferation and differentiation, apoptotic cell death, etc. TKs belong to a specific family of an enzyme that catalyses the transferring of phosphate groups from ATP to selected tyrosine residues of a target protein during the biological process to maintain the homeostasis. They work in various steps of development and progression pathways of cancer by affecting signal transduction. The aberrant and deregulated functioning of TKs results in a defective signal transduction pathway which leads to abnormality in cell transformation, proliferation, and differentiation, thus the development of cancer. Since their discovery in 1990 to date, more than 90 TKs have been reported and divided into two categories receptor and non-receptor TKs. Higher expression levels of TKs paved their status of oncoprotein and thus, they provide a potential target for the development of anti-cancer therapeutics. Here, we provided updated cancer demographic status, cancer types, and available therapeutic options targeted cancer therapeutic strategies and the role of different TKs in cancers along with recently identified molecules that target TKs. Moreover, we also included the binding interactions of chemical inhibitors with TKs.

BCS class II molecules suffer from low oral bioavailability because of their poor permeability and sub-optimal aqueous solubility. One of the approaches to enhance their bioavailability is using cyclodextrin-based nanosponges. This study aimed to optimise and evaluate the feasibility of a microwave-assisted approach to synthesise nanosponges and improve domperidone’s solubility and drug delivery potential. In the production process, microwave power level, response speed, and stirring speed were optimised using the Box-Behnken approach. Ultimately, the batch with the smallest particle size and highest yield was chosen. The optimised method of synthesis of the nanosponges resulted in a product yield of 77.4% and a particle size of 195.68 ± 2.16 nm. The nanocarriers had a drug entrapment capacity of 84 ± 4.2% and a zeta potential of −9.17± 0.43 mV. The similarity and the difference factors demonstrated proof-of-concept, showing that the drug release from the loaded nanosponges is significantly greater than the plain drug. Additionally, spectral and thermal characterisations, such as FTIR, DSC, and XRD, confirmed the entrapment of the drug within the nanocarrier. SEM scans revealed the porous nature of the nanocarriers. Microwave-assisted synthesis could be used as a better and greener approach to synthesise these nanocarriers. It could then be utilised to load drugs and improve their solubility, as seen in the case of domperidone.