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Topic Review
Mitochondrial Dynamics
Mitochondria are highly dynamic organelles that undergo morphological changes in order to adapt to cellular demands. These changes are orchestrated by the coordinated cycles of fusion and fission, referred to as mitochondrial dynamics, and dysregulation of these processes contributes to disease development. 
  • 575
  • 19 May 2021
Topic Review
Indole-Based Macrocyclization by Metal-Catalyzed Approaches
Due to its immense importance, the progress of novel approaches for the synthesis of indole-based scaffolds has increased steadily. The majority of the macrocycles synthesis proceeds through the macrolactamization and macrolactonization, as well as the C–C bond macrocyclization process described by metal-catalyzed ring-closing metathesis (RCM) and coupling reactions.
  • 575
  • 21 Jul 2023
Topic Review
Key Heterocyclic Anti-Angiogenic Leads
Pathological angiogenesis is a hallmark of cancer; accordingly, a number of anticancer FDA-approved drugs act by inhibiting angiogenesis via different mechanisms. However, the development process of the most potent anti-angiogenics has met various hurdles including redundancy, multiplicity, and development of compensatory mechanisms by which blood vessels are remodeled. Moreover, identification of broad-spectrum anti-angiogenesis targets is proved to be required to enhance the efficacy of the anti-angiogenesis drugs. In this perspective, a proper understanding of the structure activity relationship (SAR) of the recent anti-angiogenics is required. Various anti-angiogenic classes have been developed over the years; among them, the heterocyclic organic compounds come to the fore as the most promising, with several drugs approved by the FDA.
  • 573
  • 24 Feb 2021
Topic Review
Polymer-Drug Conjugate in Breast and Lung Cancer
Cancer is a chronic disease that is responsible for the high death rate, globally. The administration of anticancer drugs is one crucial approach that is employed for the treatment of cancer, although its therapeutic status is not presently satisfactory. The anticancer drugs are limited pharmacologically, resulting from the serious side effects, which could be life-threatening. Polymer drug conjugates, nano-based drug delivery systems can be utilized to protect normal body tissues from the adverse side effects of anticancer drugs and also to overcome drug resistance. They transport therapeutic agents to the target cell/tissue. 
  • 573
  • 29 Mar 2022
Topic Review
Hybrid Azine Derivatives
Infectious diseases caused by microorganisms are a major threat to human health, mostly because of drug resistance, multi-drug resistance and extensive-drug-resistance phenomena to microbial pathogens. During the past, obtaining hybrid azaheterocyclic drugs represents a powerful and attractive approach in modern antimicrobial therapy with very promising results including overcoming microbial drug resistance.
  • 569
  • 01 Dec 2022
Topic Review
HDAC8 in Different Diseases
Histone deacetylases (HDACs), also known as lysine deacetylases (KDACs), belong to the class of zinc (Zn2+)-dependent or nicotinamide adenine dinucleotide (NAD+)-dependent proteolytic enzymes. HDACs participate in transcriptional repression and chromatin condensation mechanisms by removing the acetyl moiety from the acetylated ε-amino group of histone lysines and other non-histone proteins. These enzymes play a pivotal role in the modulation of several cellular pathways such as cell proliferation, apoptosis, neurogenesis and epigenetic regulations. In some cases, HDACs are involved in the occurrence and progression of numerous pathophysiological conditions as well as diseases such as neurological disorders, fibrosis, cancer, metabolic dysfunctions and parasitic infections.
  • 568
  • 23 Sep 2022
Topic Review
Structural Changes of Hydroxylapatite during Plasma Spraying
Functional osseoconductive coatings based on hydroxylapatite (HAp) and applied preferentially by atmospheric plasma spraying to medical implant surfaces are a mainstay of modern implantology. During contact with the hot plasma jet, HAp particles melt incongruently and undergo complex dehydration and decomposition reactions that alter their phase composition and crystallographic symmetry, and thus, the physical and biological properties of the coatings. Surface analytical methods such as laser-Raman and nuclear magnetic resonance (NMR) spectroscopies are useful tools to assess the structural changes of HAp imposed by heat treatment during their flight along the hot plasma jet. 
  • 566
  • 11 Mar 2022
Topic Review
Application of Isocyanide-Based Multicomponent Reactions
Multicomponent reactions are a fascinating family of organic chemistry transformations. Traditional bimolecular reactions are outperformed by such reactions, which combine three or more reactants into one reaction product. Multicomponent reactions speed up chemical space exploration by minimizing the quantity of synthesis and refinement steps needed to create a particular target. Isocyanides (isonitriles) were the only stable organic molecules containing a formally divalent carbon atom for a long period of time. The group of isocyanides are distinguishable from other functional groups due to their reactivity.
  • 566
  • 10 May 2023
Topic Review
Sodium nitropusside a novel neuroleptic
Schizophrenia is a severe psychiatric disorder affecting up to 1% of the worldwide population. Available therapy presents different limits comprising lack of efficiency in attenuating negative symptoms and cognitive deficits, typical features of schizophrenia and severe side effects. There is pressing requirement, therefore, to develop novel neuroleptics with higher efficacy and safety. Nitric oxide (NO), an intra- and inter-cellular messenger in the brain, appears to be implicated in the pathogenesis of schizophrenia. In particular, underproduction of this gaseous molecule is associated to this mental disease. The latter suggests that increment of nitrergic activity might be of utility for the medication of schizophrenia. Based on the above, molecules able to enhance NO production, as are NO donors, might represent a class of compounds candidates. Sodium nitroprusside (SNP) is a NO donor and is proposed as a promising novel compound for the treatment of schizophrenia.
  • 565
  • 11 Oct 2021
Topic Review
Green Synthesis of Carbon Nanoparticles from Biomass
Carbon nanoparticles (CNPs) have demonstrated utility in a wide range of biological applications such as imaging, sensing and as surface-coatings. Biomass waste can be derived from either plant or animal matter as a result of processing higher-value materials, for instance leaves from trees as by product from processed wood or paper production. Biomass is abundant: trees, agriculture crops, energy crops, fruits, vegetation, wood, aquatic plants and algae, general municipal waste and animal waste.
  • 565
  • 31 Jan 2023
Topic Review
Surface Functionalization of Magnetic Nanoparticles
The surface functionalization of magnetic nanoparticles (MNPs) has witnessed significant progress recently, revolutionizing their utility in multimodal imaging, drug delivery, and catalysis. This progression, spanning over the last decade, has unfolded in discernible phases, each marked by distinct advancements and paradigm shifts. In the early stage, emphasis was placed on foundational techniques, such as ligand exchange and organic coatings, establishing the groundwork for innovations to come.
  • 565
  • 18 Oct 2023
Topic Review
Cold Plasma-Assisted Extraction of Phytochemicals
There has been growing interest in bioactive plant compounds for their beneficial effects on health and for their potential in reducing the risk of developing certain diseases such as cancer, cardiovascular diseases, and neurodegenerative disorders. The extraction techniques conventionally used to obtain these phytocompounds, however, due to the use of toxic solvents and high temperatures, tend to be supplanted by innovative and unconventional techniques, in line with the demand for environmental and economic sustainability of new chemical processes. Among non-thermal technologies, cold plasma (CP), which has been successfully used for some years in the food industry as a treatment to improve food shelf life, seems to be one of the most promising solutions in green extraction processes. CP is characterized by its low environmental impact, low cost, and better extraction yield of phytochemicals, saving time, energy, and solvents compared with other classical extraction processes. In light of these considerations, researchers aim to provide an overview of the potential and critical issues related to the use of CP in the extraction of phytochemicals, particularly polyphenols and essential oils. 
  • 565
  • 06 Sep 2023
Topic Review
Phaseolus vulgaris L. prevent Cardiovascular Diseases
The common bean (Phaseolus vulgaris L.) is known as a “new world crop”; it originated 7000 years ago in two different parts of the North and South American continents. Common beans have been highlighted as an almost perfect food due to their high content of protein, fiber, prebiotics, vitamins, and chemically diverse micronutrient composition. They have been shown to protect against oxidative stress, CVD, diabetes mellitus, metabolic syndrome, and many types of cancer. Many compounds have been identified in P. vulgaris, such as phenolic acids (chlorogenic acid, syringic acid, caffeic acid), flavonoids (kaempferol, pelargonidin, cyanidin, delphinidin), sugars, fatty acids, and tocopherols, among others.
  • 561
  • 27 Jan 2022
Topic Review
Solubility, Dissolution and Permeation Enhancement of Natural Compounds
Natural products are the major sources for drug development because of diversity in their structures. They are isolated molecules obtained from plants, minerals or animal resources and used for a variety of therapeutic purposes of human and animal diseases. Though the utilization of natural drugs is from ancient times, the drugs from natural sources still usually face drawbacks of numerous scientific evidences. Despite this, natural products present the major source of biologically active molecules and play a main role in novel drug discovery. Contrary to this, most natural products do not have characteristics of drugs and their pharmacological use is limited. Some of these characteristics lacking in natural products include low aqueous solubility, decreased dissolution rate, poor permeation and low absorption via biological membranes. The possible techniques for the dissolution/solubility and permeability improvements have been addressed which could enhance the dissolution and permeability up to several times.
  • 561
  • 17 Jun 2022
Topic Review
Anticancer Profile of Rhodanines
The rhodanine derivatives are small compounds with a broad spectrum of biological activities; they are used as antimicrobial, antiviral, antitubercular, anti-inflammatory, antidiabetic, and antitumor agents. In the pharmaceutical market, epalrestat (rhodanine-3-acetic acid) has been marketed in Japan since 1992 for treatment of diabetic complications (peripheral neuropathy). Epalrestat is an inhibitor of aldose reductase, the key enzyme in the polyol pathway of glucose metabolism under hyperglycemic conditions. The good clinical safety profile of epalrestat justified the interest of the researchers in rhodanines as potential drug candidates.
  • 561
  • 20 Jun 2022
Topic Review
Epidermal Growth Factor Receptor
Protein kinases are one of the largest enzyme families. By manipulating the location, activity, and functionality of many proteins via multisite phosphorylation, they regulate a broad spectrum of cellular processes. Numerous critical cancer processes, such as tumor growth, metastasis, neovascularization, and chemotherapy resistance, have been shown to be significantly impacted by them. Protein kinases catalyze the transfer of a phosphate group from ATP to the hydroxy group of an amino acid residue. In cellular and molecular process, protein kinases are indispensable. As a result, they play a crucial part in the growth, dissemination, and survival of tumor cells in humans. Hence, this class of enzymes has drawn significant attention as a potential therapeutic target, with multiple kinase suppressors now receiving FDA approval for different cancer indications.
  • 561
  • 25 Mar 2024
Topic Review
Synthesis of Metal Complexes of 2-Thiouracil and Derivatives
The thionamide antithyroid agents were discovered largely through observations carried out by various researchers in the 1940s that found that sulfhydryl-containing substances were goitrogenic in animals. Prof. Edwin B. Astwood started using these drugs to treat hyperthyroidism. The development background of these agents, the coordination possibility of 2-thiouracil and its derivatives are presented herein.
  • 559
  • 12 Apr 2024
Topic Review
EGFR-Targeted Pentacyclic Triterpene Analogues for Glioma Therapy
Glioma, particularly its most malignant form, glioblastoma multiforme (GBM), is the most common and aggressive malignant central nervous system tumor. The drawbacks of the current chemotherapy for GBM have aroused curiosity in the search for targeted therapies. Aberrantly overexpressed epidermal growth factor receptor (EGFR) in GBM results in poor prognosis, low survival rates, poor responses to therapy and recurrence, and therefore EGFR-targeted therapy stands out as a promising approach for the treatment of gliomas. In this context, a series of pentacyclic triterpene analogues were subjected to in vitro and in silico assays, which were conducted to assess their potency as EGFR-targeted anti-glioma agents. In particular, compound 10 was the most potent anti-glioma agent with an IC50 value of 5.82 µM towards U251 human glioblastoma cells. Taking into account its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), compound 10 exerts selective antitumor action towards Jurkat human leukemic T-cells. This compound also induced apoptosis and inhibited EGFR with an IC50 value of 9.43 µM compared to erlotinib (IC50 = 0.06 µM). Based on in vitro and in silico data, compound 10 stands out as a potential orally bioavailable EGFR-targeted anti-glioma agent endowed with the ability to cross the blood–brain barrier (BBB).
  • 557
  • 03 Nov 2021
Topic Review
Synthetic Methodologies of Indole-3-Carbinol
Indole-3-Carbinol (I3C)  is an important phytochemical contained in cruciferous vegetables and is able to exert various activities among which are cardioprotective, antioxidant, anti-inflammatory, antiangiogenesis, and antimicrobial activities, the promotion of tumor cell apoptosis and, an important inhibition of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS)-CoV-2 viral egression, including the Omicron variant.
  • 554
  • 24 May 2023
Topic Review
Magnetic Drug-Delivery System
Magnetic nanoparticles (MNPs) are nanoscale particles (1–100 nm) that can be guided through an external magnetic field due to their superparamagnetic, ferrimagnetic, and ferromagnetic properties, which may provide features for biomedical applications. 
  • 553
  • 23 Aug 2022
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