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Topic Review
Gemcitabine Peptide-Based Conjugates
Gemcitabine is an anticancer drug used to treat a wide range of solid tumors and is a first-line treatment for pancreatic cancer. The effect of gemcitabine is significantly weakened by its rapid plasma degradation. In addition, the systemic toxicity and drug resistance significantly reduce its chemotherapeutic efficacy. Up to now, many approaches have been made to improve the therapeutic index of gemcitabine. One of the recently developed approaches to improve conventional chemotherapy is based on the direct targeting of chemotherapeutics to cancer cells using the peptide-drug conjugates (PDCs).
  • 1.5K
  • 24 Feb 2021
Topic Review
Development of CDK4/6 Inhibitors
CDKs, a family of serine/threonine kinases, regulate cell cycle progression into the four distinct phases G1, S (DNA synthesis), G2 and M, and are crucially involved in the regulation of cell division and proliferation.
  • 1.5K
  • 23 Apr 2021
Topic Review
Synthesis of 3,4-Dihydropyrimidin(thio)one Containing Scaffold
The interest in 3,4-dihydropyrimidine-2(1H)-(thio)ones is increasing every day, mainly due to their paramount biological relevance. The Biginelli reaction is the classical approach to reaching these scaffolds, although the product diversity suffers from some limitations. In order to overcome these restrictions, two main approaches have been devised. The first one involves the modification of the conventional components of the Biginelli reaction and the second one refers to the postmodification of the Biginelli products. Both strategies have been extensively revised in this manuscript. Regarding the first one, initially, the modification of one of the components was covered. Although examples of modifications of the three of them were described, by far the modification of the keto ester counterpart was the most popular approach, and a wide variety of different enolizable carbonylic compounds were used; moreover, changes in two or the three components were also described, broadening the substitution of the final dihydropyrimidines. Together with these modifications, the use of Biginelli adducts as a starting point for further modification was also a very useful strategy to decorate the final heterocyclic structure.
  • 1.5K
  • 15 Aug 2022
Topic Review
Pyrazino[1,2-a]Indoles
The pyrazino[1,2-a]indole unit is a tricyclic aromatic nucleus combining an indole and a pyrazine linked by the N5 and C9a atoms. The Synthesis and Biological Activities of Pyrazino[1,2-a]Indole and Pyrazino[1,2-a]Indol-1-One Derivatives is presented.
  • 1.5K
  • 10 Aug 2021
Topic Review
Dapsone Imine Derivatives
Dapsone (DDS) is an antibacterial drug with well-known antioxidant properties. However, the antioxidant behavior of its derivatives has not been well explored. In the present work, the antioxidant activity of 10 dapsone derivatives 4-substituted was determined by an evaluation in two in vitro models (DPPH radical scavenging assay and ferric reducing antioxidant power). These imine derivatives 1–10 were obtained through condensation between DDS and the corresponding aromatic aldehydes 4-substuited. Three derivatives presented better results than DDS in the determination of DPPH (2, 9, and 10). Likewise, we have three compounds with better reducing activity than dapsone (4, 9, and 10). In order to be more insight, the redox process, a conceptual DFT analysis was carried out. Molecular descriptors such as electronic distribution, the total charge accepting/donating capacity (I/A), and the partial charge accepting/donating capacity (ω+/ω−) were calculated to analyze the relative donor-acceptor capacity through employing a donor acceptor map (DAM). The DFT calculation allowed us to establish a relationship between GAPHOMO-LUMO and DAM with the observed antioxidant effects. According to the results, we concluded that compounds 2 and 3 have the lowest Ra values, representing a good antioxidant behavior observed experimentally in DPPH radical capturing. On the other hand, derivatives 4, 9, and 10 display the best reducing capacity activity with the highest ω− and Rd values. Consequently, we propose these compounds as the best antireductants in our DDS imine derivative series.
  • 1.5K
  • 08 Oct 2021
Topic Review
Tragia L. Genus
Tragia L. is a genus of plants belonging to the Euphorbiaceae family with worldwide intertropical distribution, composed of more than 150 species.
  • 1.5K
  • 16 May 2022
Topic Review
Monoterpenes as Anticancer Therapeutic Agents
Terpenes—a diverse group of secondary metabolites—constitute the largest class of natural products abundant in almost every plant species.
  • 1.5K
  • 17 May 2021
Topic Review
Use of Kojic Acid in Cosmetics
In 1907, Saito discovered Kojic Acid (KA), a natural product; it has since become one of the most investigated skin-lightening agents. KA inhibits tyrosinase and has been commonly researched in the cosmetic industry. It is incorporated in many kinds of cosmetic products.
  • 1.4K
  • 23 Jun 2022
Topic Review
Common Genera of Cyanobacteria and Their Characteristics
Blue-green algae, or cyanobacteria, may be prevalent in our rivers and tap water. These minuscule bacteria can grow swiftly and form blooms in warm, nutrient-rich water. 
  • 1.4K
  • 27 Sep 2023
Topic Review
G-Quadruplexes: Emerging Anticancer Roles
G-quadruplexes, a family of (thermodynamically and kinetically stable) tetraplex helices, are non-canonical secondary structures derived from guanine (G)-rich sequences of nucleic acids. G-quadruplexes were found to occur in functionally-important regions of the human genome, including the telomere tandem sequences, several proto-oncogene promoters and other regulatory regions, ribosomal DNA (rDNA), as well as mRNA sequences encoding for proteins with roles in tumorigenesis, thus establishing a clear connection between G-quadruplexes and known hallmarks of cancer. Stabilization of G-quadruplexes belonging to the above categories, by means of small-molecule intervention, has been correlated with a range of anticancer effects, which has led to classifying G-quadruplexes as novel potential targets in anticancer research. The most common ways in which G-quadruplexes are now understood to serve in an anticancer capacity are presented herein.
  • 1.4K
  • 03 Mar 2021
Topic Review
Chemistry of Essential Oils
The term essential oil was created in the 16th century and refers to the theory of “Quinta essentia” proposed by the famous German-Swiss alchemist and physician Paracelsus (1493–1541), born by Theophrastus Philippus Aureolus Bombastus von Hohenheim.
  • 1.4K
  • 13 Oct 2023
Topic Review
Alzheimer's disease
Alzheimer's disease (AD) is a multifactorial disease and the most common neurodegenerative disorder affecting the elderly population world-wide.The used medications treat the symptoms of AD, but without any delay on the progression of the disease. Curcumin presented favorable effects on AD. In the last decade curcumin analogues and derivatives have been synthesized in an attempt to optimize the beneficial properties of curcumin and improve its absorbance and  distribution per os as a therapeutic agent. Reviewing the bibliographical data of the last decade, information on the structures and / or chemical groups that are associated with specific action against AD, was gathered, derived from docking studies, (Q)SAR from vitro and in vivo tests. Phenolic hydroxyl groups might contribute to the anti-amyloidogenic activity. Phenyl methoxy groups seems to contribute to the suppression of Aβ42 and to the suppression of APP. Hydrophobic interactions revealed to be important. The presence of flexible moieties at the linker are crucial for the inhibition of Aβ aggregation. The inhibitory activity of derivatives is increased with the expansion of the aromatic rings. The keto-enol tautomer form offers as a new modification for the design of amyloid-binding agents. Taking the above under consideration  innovative design  and synthesis will lead to more potent and specific curcumin analogues and derivatives against AD.
  • 1.4K
  • 30 Oct 2020
Topic Review
Antioxidant Compounds Extracted from Plants for Vegetable Oils
Oil oxidation is the main factor limiting vegetable oils’ quality during storage, as it leads to the deterioration of oil’s nutritional quality and gives rise to disagreeable flavors. These changes make fat-containing foods less acceptable to consumers. To deal with this problem and to meet consumer demand for natural foods, vegetable oil fabricators and the food industry are looking for alternatives to synthetic antioxidants to protect oils from oxidation. In this context, natural antioxidant compounds extracted from different parts (leaves, roots, flowers, and seeds) of medicinal and aromatic plants (MAPs) could be used as a promising and sustainable solution to protect consumers’ health. 
  • 1.4K
  • 21 Nov 2022
Topic Review
Plant-Based Indole Alkaloids
Indole (C8H7N) is a weakly basic molecule consisting of a pyrrole ring fused to a benzene nucleus, and ten π electrons move throughout the structure. The basic environment of indole alkaloids is thought to be caused by the delocalization of the lone pair of nitrogen electrons into the free circulation of the π electronic system. This results in indole becoming protonated at the C-3 position, which is thermodynamically more stable.Indole alkaloids have gained popularity due to their diverse pharmacological activities. Indole alkaloids have been identified in several prominent plant families, including Apocynaceae, Rubiaceae, Nyssaceae, and Loganiaceae, among others. Some of the identified indole alkaloid compounds have been highly effective in pre-clinical and clinical studies. Thousands of compounds containing the indole nucleus have been isolated from plant sources. Their pharmacological activities were assessed, with some now being examined in clinical trials and some already approved for therapeutic use in humans. Indole alkaloids are often characterized by their potent biological activities, which are relevant to the field of medicine, including anticancer, antibacterial, antiviral, antimalarial, antifungal, anti-inflammatory, antidepressant, analgesic, hypotensive, anticholinesterase, antiplatelet, antidiarrheal, spasmolytic, antileishmanial, lipid-lowering, antimycobacterial, and antidiabetic activities. 
  • 1.4K
  • 27 Apr 2021
Topic Review
Antagonists of the AT1receptor
Antagonists of the AT1receptor (AT1R) are beneficial molecules that can prevent the peptide hormone angiotensin II from binding and activating the specific receptor causing hypertension in pathological states.
  • 1.4K
  • 06 Jan 2021
Topic Review
Antibacterial Activity of Heterocyclic Compounds
Heterocyclic compounds are cyclic compounds which contain the atoms of two discrete elements as representative of their ring(s). They belong to one of the larger classes of organic compounds and also appear more valuable in different fields of chemistry.
  • 1.3K
  • 19 Dec 2022
Topic Review
Ethiopian Anticancer Plants
This entry provides an overview on the active phytochemical constituents of twenty-seven medicinal plants that are traditionally used to manage cancer in Ethiopia. It is compiled and discusses the potential anticancer, antiproliferative, and cytotoxic agents based on the types of secondary metabolites, such as terpenoids, phenolic compounds, alkaloids, steroids, and lignans. Among the anticancer secondary metabolites reported in this review, only few have been isolated from plants that are originated and collected in Ethiopia, and the majority of compounds are reported from plants belonging to different areas of the world. Thus, based on the available bioactivity reports, extensive and more elaborate ethnopharmacology-based bioassay-guided studies have to be conducted on selected traditionally claimed Ethiopian anticancer plants, which inherited from a unique and diverse landscape, with the aim of opening a way forward to conduct anticancer drug discovery program.
  • 1.3K
  • 21 Oct 2020
Topic Review
Covalent Inhibitors for Neglected Diseases
Neglected Tropical Diseases (NTD) is a group of 20 diseases affecting more than 1 billion people in the world, especially those living in poor communities of tropical areas. Caused by a variety of etiologic agents such as viruses, bacteria, and parasites, these diseases have a great impact on public health, with social and economic consequences to the affected populations.
  • 1.3K
  • 24 Jul 2023
Topic Review
Organoboron Compounds
The unique electron deficiency and coordination property of boron led to a wide range of applications in chemistry, energy research, materials science and the life sciences. The use of boron-containing compounds as pharmaceutical agents has a long history, and recent developments have produced encouraging strides. Boron agents have been used for both radiotherapy and chemotherapy. In radiotherapy, boron neutron capture therapy (BNCT) has been investigated to treat various types of tumors, such as glioblastoma multiforme (GBM) of brain, head and neck tumors, etc. Boron agents playing essential roles in such treatments and other well-established areas have been discussed elsewhere. Organoboron compounds used to treat various diseases besides tumor treatments through BNCT technology have also marked an important milestone. Following the clinical introduction of bortezomib as an anti-cancer agent, benzoxaborole drugs, tavaborole and crisaborole, have been approved for clinical use in the treatments of onychomycosis and atopic dermatitis. Some heterocyclic organoboron compounds represent potentially promising candidates for anti-infective drugs.
  • 1.3K
  • 25 Jun 2021
Topic Review
Ligands for Alzheimer’s Disease therapy
Despite tremendous research efforts at every level, globally, there is still a lack of effectivedrugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastatingneurodegenerative disease are not yet clearly understood. This review analyses the relevance ofmultiple ligands in drug discovery for AD as a versatile toolbox for a polypharmacological approachto AD. Herein, we highlight major targets associated with AD, ranging from acetylcholine esterase(AChE), beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), glycogen synthase kinase3 beta ( GSK-3β), N-methyl-D-aspartate (NMDA) receptor, monoamine oxidases (MAOs), metal ions inthe brain, 5-hydroxytryptamine (5-HT) receptors, the third subtype of histamine receptor (H3 receptor),to phosphodiesterases (PDEs), along with a summary of their respective relationship to the diseasenetwork. In addition, a multitarget strategy for AD is presented, based on reported milestones in thisarea and the recent progress that has been achieved with multitargeted-directed ligands (MTDLs).Finally, the latest publications referencing the enlarged panel of new biological targets for AD relatedto the microglia are highlighted. However, the question of how to find meaningful combinations oftargets for an MTDLs approach remains unanswered.
  • 1.3K
  • 04 Aug 2020
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