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Topic Review
Biography
Topic Review
Taxol Biosynthetic Pathway
Taxol is one of the most effective anticancer drugs in the world that is widely used in the treatment of several cancers. The elucidation of the taxol biosynthetic pathway is the key to solve the problem of taxol supply. So far, the taxol biosynthetic pathway has been reported to require an estimated 20 steps of enzymatic reactions, and most of enzymes involved have been well characterized. In details, the source and formation of the taxane core and the process of the downstream synthetic pathway have been basically depicted, while the modification of the core taxane skeleton has not been fully reported, mainly concerning the developments from diol intermediates to 2-debenzoyltaxane.
1.6K
01 Jun 2021
Topic Review
Targeting Nrf2 and NF-κB Signaling Pathways in Cancer
Plant secondary metabolites, known as phytochemicals, have gained much attention in light of the “circular economy”, to reutilize waste products deriving from agriculture and food industry. Phytochemicals are known for their onco-preventive and chemoprotective effects, among several other beneficial properties. Apple phytochemicals have been extensively studied for their effectiveness in a wide range of diseases, cancer included.
280
15 Feb 2023
Topic Review
Taccalonolides
Taccalonolides are a new class of microtube-stabilizing agents isolated from plants of the genus Tacca demonstrating effectiveness against drug-resistant tumors in cellular and animal models.
451
16 Sep 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.
306
24 May 2023
Topic Review
Synthetic Imidazopyridine-Based Derivatives
Fused pyridines are reported to display various pharmacological activities, such as antipyretic, analgesic, antiprotozoal, antibacterial, antitumor, antifungal, anti-inflammatory, and antiapoptotic. They are widely used in the field of medicinal chemistry. Imidazopyridines (IZPs) are crucial classes of fused heterocycles that are expansively reported on in the literature. Evidence suggests that IZPs, as fused scaffolds, possess more diverse profiles than individual imidazole and pyridine moieties. Bacterial infections and antibacterial resistance are ever-growing risks in the 21st century. Only one IZP, i.e., rifaximin, is available on the market as an antibiotic
450
02 Feb 2023
Topic Review
Synthetic Hemorphin Analogs Containing Non-Natural Amino Acids
The endogenous hemorphins are bioactive peptides with activity on opioid receptors. Several research teams have synthesized, characterized, and pharmacologically evaluated synthetic hemorphin analogs containing unusual amino acids, D-amino acids, α-aminophosphonic acids, and their derivatives. Research focuses on the structure-activity relationship analysis, details on specific methods for their characterization, and the advantage of synthetic hemorphin analogs compared to endogenous peptides as potent biologically active compounds with a complex mechanism of action.
594
05 Dec 2022
Topic Review
Synthesis of nucleobase-modified RNA oligonucleotides
The review summarizes the methods of site-specific incorporation of nucleobase-modified units into RNA oligomers via the post-synthetic strategy including recently discovered native hypermodified functional groups, fluorescent dyes, photoreactive groups, disulfide crosslinks, and nitroxide spin labels.
1.6K
06 Aug 2020
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.
75
12 Apr 2024
Topic Review
Synthesis of Metabolite of Resveratrol by Beauveria bassiana
Resveratrol is a well-known dietary polyphenol because it has a variety of beneficial biological activities. The fungus Beauveria bassiana is one of the most frequently used microorganisms for the biotransformation of polyphenols. Recently, resvebassianol A (2), a glycosylated metabolite of resveratrol by B. bassiana, was isolated and structurally elucidated. It was demonstrated to exhibit antioxidant, regenerative, and anti-inflammatory activities with no cytotoxicity. Here, we report the first total synthesis of resvebassianol A, 4'-O-β-(4'"-O-methylglucopyranosyl)resveratrol (2), and its regiomer, 3-O-β-(4 -O-methylglucopyranosyl)resveratrol (3). Key reactions include (i) the construction of a stilbene core via a novel Heck reaction of aryl halides and styrenes, and (ii) glycosylation with unnatural methylglucopyranosyl bromide. The glycosylation step was carefully optimized by varying the bases and solvents. Resveratrol metabolites 2 and 3 were obtained at 7.5% and 6.3% of the overall yield, respectively.
565
25 Oct 2021
Topic Review
Synthesis of Mesoporous Silica Nanoparticles
Mesoporous silica nanoparticles (MSNs) have been advocated as nanocarriers for the treatment of various diseases because of their physicochemical properties and biocompatibility. The use of MSNs combined with therapeutic agents can provide better encapsulation and effective delivery. MSNs as nanocarriers might also be a promising tool to lower the therapeutic dosage levels and thereby to reduce undesired side effects. Furthermore, when combined with imaging compounds for diagnosis, they can be employed as theragnostic agents thus allowing both imaging and therapy using the same nanoparticle.
839
19 Jul 2023
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