Tryptamine–Triazole Hybrid Compounds for Selective Butyrylcholinesterase Inhibition

2019 ◽  
Vol 40 (6) ◽  
pp. 544-553
Author(s):  
Minky Son ◽  
Haneul Lee ◽  
Cheolmin Jeon ◽  
Yujung Kang ◽  
Chanin Park ◽  
...  
Keyword(s):  
Hybrid Compounds ◽  
Butyrylcholinesterase Inhibition

Hybrid Compounds & Oxidative Stress Induced Apoptosis in Cancer Therapy

2020 ◽  
Vol 27 (13) ◽  
pp. 2118-2132 ◽  
Author(s):  
Aysegul Hanikoglu ◽  
Hakan Ozben ◽  
Ferhat Hanikoglu ◽  
Tomris Ozben
Keyword(s):  
Oxidative Stress ◽  
Drug Resistance ◽  
Side Effects ◽  
Cancer Therapy ◽  
Tumor Cells ◽  
Anticancer Drugs ◽  
Chemotherapeutic Agents ◽  
Oxidation Reactions ◽  
Hybrid Compounds ◽  
Induced Apoptosis

: Elevated Reactive Oxygen Species (ROS) generated by the conventional cancer therapies and the endogenous production of ROS have been observed in various types of cancers. In contrast to the harmful effects of oxidative stress in different pathologies other than cancer, ROS can speed anti-tumorigenic signaling and cause apoptosis of tumor cells via oxidative stress as demonstrated in several studies. The primary actions of antioxidants in cells are to provide a redox balance between reduction-oxidation reactions. Antioxidants in tumor cells can scavenge excess ROS, causing resistance to ROS induced apoptosis. Various chemotherapeutic drugs, in their clinical use, have evoked drug resistance and serious side effects. Consequently, drugs having single-targets are not able to provide an effective cancer therapy. Recently, developed hybrid anticancer drugs promise great therapeutic advantages due to their capacity to overcome the limitations encountered with conventional chemotherapeutic agents. Hybrid compounds have advantages in comparison to the single cancer drugs which have usually low solubility, adverse side effects, and drug resistance. This review addresses two important treatments strategies in cancer therapy: oxidative stress induced apoptosis and hybrid anticancer drugs.

Hybrid Compounds as Anti-infective Agents

2017 ◽  
Vol 17 (9) ◽  
pp. 1080-1095 ◽  
Author(s):  
María Sbaraglini ◽  
Alan Talevi
Keyword(s):  
Hybrid Compounds

scholarly journals Meroterpenoids: A Comprehensive Update Insight on Structural Diversity and Biology

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 957
Author(s):  
Mamona Nazir ◽  
Muhammad Saleem ◽  
Muhammad Imran Tousif ◽  
Muhammad Aijaz Anwar ◽  
Frank Surup ◽  
...  
Keyword(s):  
Amino Acids ◽  
Secondary Metabolites ◽  
Biological Effects ◽  
Structural Diversity ◽  
Chemical Diversity ◽  
Biosynthetic Pathways ◽  
Natural Sources ◽  
Hybrid Compounds ◽  
Anti Inflammatory

Meroterpenoids are secondary metabolites formed due to mixed biosynthetic pathways which are produced in part from a terpenoid co-substrate. These mixed biosynthetically hybrid compounds are widely produced by bacteria, algae, plants, and animals. Notably amazing chemical diversity is generated among meroterpenoids via a combination of terpenoid scaffolds with polyketides, alkaloids, phenols, and amino acids. This review deals with the isolation, chemical diversity, and biological effects of 452 new meroterpenoids reported from natural sources from January 2016 to December 2020. Most of the meroterpenoids possess antimicrobial, cytotoxic, antioxidant, anti-inflammatory, antiviral, enzyme inhibitory, and immunosupressive effects.

scholarly journals Novel Hybrid Compounds Containing Benzofuroxan and Aminothiazole Scaffolds: Synthesis and Evaluation of Their Anticancer Activity

2021 ◽  
Vol 22 (14) ◽  
pp. 7497
Author(s):  
Elena Chugunova ◽  
Gabriele Micheletti ◽  
Dario Telese ◽  
Carla Boga ◽  
Daut Islamov ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Normal Liver ◽  
Mitochondrial Pathway ◽  
Reaction Pathways ◽  
Aromatic Nucleophilic Substitution ◽  
X Ray ◽  
Hybrid Compounds ◽  
Aromatic Nucleophilic Substitution Reaction ◽  
Further Development

A series of novel hybrid compounds containing benzofuroxan and 2-aminothiazole moieties are synthesized via aromatic nucleophilic substitution reaction. Possible reaction pathways have been considered quantum-chemically, which allowed us to suggest the most probable products. The quantum chemical results have been proved by X-ray data on one compound belonging to the synthesized series. It was shown that the introduction of substituents to both the thiazole and amine moieties of the compounds under study strongly influences their UV/Vis spectra. Initial substances and obtained hybrid compounds have been tested in vitro as anticancer agents. Target compounds showed selectivity towards M-HeLa tumor cell lines and were found to be more active than starting benzofuroxan and aminothiazoles. Furthermore, they are considerably less toxic to normal liver cells compared to Тamoxifen. The mechanism of action of the studied compounds can be associated with the induction of apoptosis, which proceeds along the mitochondrial pathway. Thus, new hybrids of benzofuroxan are promising candidates for further development as anticancer agents.

scholarly journals Modified Nucleosides, Nucleotides and Nucleic Acids via Click Azide-Alkyne Cycloaddition for Pharmacological Applications

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3100
Author(s):  
Daniela Perrone ◽  
Elena Marchesi ◽  
Lorenzo Preti ◽  
Maria Luisa Navacchia
Keyword(s):  
Cancer Therapy ◽  
Nucleic Acids ◽  
Click Chemistry ◽  
Nucleoside Analogs ◽  
Modified Nucleosides ◽  
Biological Molecules ◽  
Dipolar Cycloaddition ◽  
Virus Diseases ◽  
Reaction Conditions ◽  
Hybrid Compounds

The click azide = alkyne 1,3-dipolar cycloaddition (click chemistry) has become the approach of choice for bioconjugations in medicinal chemistry, providing facile reaction conditions amenable to both small and biological molecules. Many nucleoside analogs are known for their marked impact in cancer therapy and for the treatment of virus diseases and new targeted oligonucleotides have been developed for different purposes. The click chemistry allowing the tolerated union between units with a wide diversity of functional groups represents a robust means of designing new hybrid compounds with an extraordinary diversity of applications. This review provides an overview of the most recent works related to the use of click chemistry methodology in the field of nucleosides, nucleotides and nucleic acids for pharmacological applications.

scholarly journals Chloroquine and Sulfadoxine Derivatives Inhibit ZIKV Replication in Cervical Cells

Viruses ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 36
Author(s):  
Audrien Alves Andrade de Souza ◽  
Lauana Ribas Torres ◽  
Lyana Rodrigues Pinto Lima Capobianco ◽  
Vanessa Salete de Paula ◽  
Cynthia Machado Cascabulho ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Specific Treatment ◽  
Vero Cells ◽  
Vehicle Control ◽  
Therapeutic Window ◽  
Chemical Structures ◽  
Hybrid Compounds ◽  
Cervical Cells ◽  
Zika Fever

Despite the severe morbidity caused by Zika fever, its specific treatment is still a challenge for public health. Several research groups have investigated the drug repurposing of chloroquine. However, the highly toxic side effect induced by chloroquine paves the way for the improvement of this drug for use in Zika fever clinics. Our aim is to evaluate the anti-Zika virus (ZIKV) effect of hybrid compounds derived from chloroquine and sulfadoxine antimalarial drugs. The antiviral activity of hybrid compounds (C-Sd1 to C-Sd7) was assessed in an in-vitro model of human cervical and Vero cell lines infected with a Brazilian (BR) ZIKV strain. First, we evaluated the cytotoxic effect on cultures treated with up to 200 µM of C-Sds and observed CC50 values that ranged from 112.0 ± 1.8 to >200 µM in cervical cells and 43.2 ± 0.4 to 143.0 ± 1.3 µM in Vero cells. Then, the cultures were ZIKV-infected and treated with up to 25 µM of C-Sds for 48 h. The treatment of cervical cells with C-Sds at 12 µM induced a reduction of 79.8% ± 4.2% to 90.7% ± 1.5% of ZIKV–envelope glycoprotein expression in infected cells as compared to 36.8% ± 2.9% of infection in vehicle control. The viral load was also investigated and revealed a reduction of 2- to 3-logs of ZIKV genome copies/mL in culture supernatants compared to 6.7 ± 0.7 × 108 copies/mL in vehicle control. The dose–response curve by plaque-forming reduction (PFR) in cervical cells revealed a potent dose-dependent activity of C-Sds in inhibiting ZIKV replication, with PFR above 50% and 90% at 6 and 12 µM, respectively, while 25 µM inhibited 100% of viral progeny. The treatment of Vero cells at 12 µM led to 100% PFR, confirming the C-Sds activity in another cell type. Regarding effective concentration in cervical cells, the EC50 values ranged from 3.2 ± 0.1 to 5.0 ± 0.2 µM, and the EC90 values ranged from 7.2 ± 0.1 to 11.6 ± 0.1 µM, with selectivity index above 40 for most C-Sds, showing a good therapeutic window. Here, our aim is to investigate the anti-ZIKV activity of new hybrid compounds that show highly potent efficacy as inhibitors of ZIKV in-vitro infection. However, further studies will be needed to investigate whether these new chemical structures can lead to the improvement of chloroquine antiviral activity.

Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities

2003 ◽  
Vol 11 (10) ◽  
pp. 2163-2174 ◽  
Author(s):  
Sven Graßmann ◽  
Joachim Apelt ◽  
Wolfgang Sippl ◽  
Xavier Ligneau ◽  
Heinz H Pertz ◽  
...  
Keyword(s):  
Imidazole Derivatives ◽  
Hybrid Compounds

Diterpenoid and phenolic contents of Sideritis hololeuca Boiss & Heldr. Apud Bentham with antioxidant and anticholinesterase activity

2020 ◽  
Vol 75 (5-6) ◽  
pp. 161-169
Author(s):  
Sema Carikci ◽  
Ahmet C. Goren ◽  
Turgut Kilic
Keyword(s):  
Essential Oil ◽  
Biological Activities ◽  
Reducing Power ◽  
Acetone Extract ◽  
Inhibition Activity ◽  
Phenolic Contents ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Main Component ◽  
Butyrylcholinesterase Inhibition

AbstractThe objective of this study is to determine essential oil, diterpenoid and phenolic contents of Sideritis hololeuca along with their biological activities. Phytol was found to be the main component of the essential oil. Seven known kaurane diterpenoids, siderol (140 mg, 0.16%, w/w), 7-acetoxy sideroxol (15 mg, 0.02%, w/w), eubol (6 mg, 0.01%, w/w), eubotriol (5 mg, 0.03%, w/w), 7-epicandicandiol (3 mg, 0.02%, w/w), ent-7α-acetoxy-18-hydroxykaur-16-ene (5 mg, 0.01%, w/w) and linearol [by liquid chromatography-tandem mass spectrometry (LC-MS/MS)] were determined from the species. Moreover, vanillin (21 mg, 0.10%, w/w), which was not isolated from any Sideritis species earlier, was isolated from an acetone extract of S. hololeuca. Quantitative amounts of some phenolic compounds in n-hexane, dichloromethane, acetone, methanol extracts and infusion and decoction of the plants were also investigated by LC-MS/MS. Antioxidant capacity and acetylcholinesterase, butyrylcholinesterase inhibition effects of the species were evaluated. The extracts of methanol and infusion and decoction of species showed moderate butyrylcholinesterase inhibition activity. The highest inhibition was observed from the decoction of species. The Cu2+ reducing power of infusion was determined as 1.435 mmol TR g−1.

Sign in / Sign up

Export Citation Format

Share Document