scholarly journals Synthesis and Anticancer Activity of Some New Derivatives of Coumarin and Quinolinyl Mercaptotriazoles

2012 ◽  
Vol 9 (4) ◽  
pp. 1737-1745 ◽  
Author(s):  
Mona A. Hosny ◽  
Hyam A. Radwan ◽  
Emtithal A. El-Sawi
Keyword(s):  
Anticancer Activity ◽  
Mass Spectra ◽  
Anhydrous Pyridine ◽  
Coumarin Derivatives ◽  
Anticancer Activities ◽  
Pechmann Condensation ◽  
Montmorillonite Clays ◽  
Derivatives Of

Pechmann condensation of ethylacetoacetate with derivatives of phenol by heating in absence of solvent and with montmorillonite clays K-10 afforded coumarin derivatives(1a-e)in good yields which on reaction with thiosemicarbazide in anhydrous pyridine yielded coumarin-quinolinyl mercaptotriazole(2a-e). The latter compounds were evaluated for their antimicrobial and anticancer activities. The newly synthesized compounds were characterized by IR,1HNMR and mass spectra.

Design, Synthesis and Evaluation of Antioxidant Activity of Some Coumarin Derivatives

2019 ◽  
Vol 4 (3) ◽  
pp. 138-143
Author(s):  
R.D. Ukirde ◽  
R.B. Patil ◽  
S.D. Sawant
Keyword(s):  
Antioxidant Activity ◽  
Heterocyclic Compounds ◽  
Coumarin Derivatives ◽  
Phosphoryl Chloride ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Derivatives Of ◽  
Substituted Coumarins ◽  
In Vitro Antioxidant Activity

Coumarin derivatives are an important class of heterocyclic compounds, specifically 4-amino substituted coumarins with antioxidant, anticancer activities. The above observations prompted us to synthesize new coumarins with various substitutions. The starting material 4-chloro-2H-chromen-2-one was synthesized by refluxing a mixture of 4-hydroxy-2H-chromen-2-one in phosphoryl chloride. The 4-substituted amine derivatives of coumarin were synthesized by refluxing 4-chloro-2H-chromen-2- one with 4-substituted amines and anhydrous K2CO3 and methanol. All the eleven 4-substituted amine derivatives of coumarin were synthesized by replacing chloro group with different amines. These coumarin derivatives were evaluated for in vitro antioxidant activity using quercetin as standard.

Design, synthesis, anticancer activity and mechanism studies of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid

2022 ◽  
Author(s):  
Wen-Yan Wang ◽  
Zihui Yang ◽  
A-Liang Li ◽  
Qing-Song Liu ◽  
Yue Sun ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Ursolic Acid ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Derivatives Of ◽  
Mcf 7

A series of novel 2-amino-4-aryl-pyrimidine derivatives of ursolic acid were designed, synthesized, and evaluated for their anticancer activities against four cancer cell lines (MCF-7, HeLa, HepG2, and A549) and a...

scholarly journals Synthesis, Test of Antioxidant and Anticancer Activities Flavonol 2- (3,4,5-Dimethoxyphenyli) -3-Hydroxy-4H-Chromen-4-On

2019 ◽  
Vol 17 (2) ◽  
pp. 16
Author(s):  
Muhamad Rokim ◽  
Adel Zamri ◽  
Hilwan Yuda Teruna
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Spectroscopic Data ◽  
Dpph Assay ◽  
Anticancer Activities ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Mts Assay

Flavonols 2-(3,4,5-dimethoxyphenyli)-3-hydroxy-4h-chromen-4-on) derivatives of 2'-hydroxycalone have been synthesized under basic condition (KOH). The structures of all compounds were characterized based on the interpretation of spectroscopic data including UV, FTIR, NMR and HRMS. Antioxidant activity was evaluated using the DPPH assay and anticancer activity was evaluated using the MTS assay which showed that the flavonol 2'-hydroxycalone derivative was potentially active as antioxidants and anticancer with IC50 values <1000 µg / mL.

Recent Advances in the Synthesis of Coumarin Derivatives via Pechmann Condensation

2016 ◽  
Vol 20 (7) ◽  
pp. 798-828 ◽  
Author(s):  
Abhay S. Zambare ◽  
Firoz A. Kalam Khan ◽  
Sureshchandra P. Zambare ◽  
Shantanu D. Shinde ◽  
Jaiprakash N. Sangshetti
Keyword(s):  
Coumarin Derivatives ◽  
Pechmann Condensation ◽  
Recent Advances

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides

2019 ◽  
Vol 19 (13) ◽  
pp. 1093-1110 ◽  
Author(s):  
Adel A.H. Abdel Rahman ◽  
Ibrahim F. Nassar ◽  
Amira K.F. Shaban ◽  
Dina S. EL-Kady ◽  
Hanem M. Awad ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Human Liver ◽  
Docking Studies ◽  
Cyclin Dependent Kinase ◽  
Binding Interaction ◽  
Enzyme Active Site ◽  
Human Liver Cancer ◽  
Amino Derivatives ◽  
Activity Behavior ◽  
Derivatives Of

Background & Objective:New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.Methods:The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.Results:The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.Conclusion:Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.

Anticancer Activity and Topoisomerase II Inhibition of Naphthalimides with ω-Hydroxylalkylamine Side-Chains of Different Lengths

2019 ◽  
Vol 15 (5) ◽  
pp. 550-560
Author(s):  
Mateusz D. Tomczyk ◽  
Anna Byczek-Wyrostek ◽  
Klaudia Strama ◽  
Martyna Wawszków ◽  
Przemysław Kasprzycki ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Inhibitory Activity ◽  
Topoisomerase Ii ◽  
Significant Activity ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
Substitution Pattern ◽  
Topo Ii

Background: The substituted 1,8-Naphthalimides (1H-benzo[de]isoquinoline-1,3(2H)- diones) are known as DNA intercalators stabilizing DNA-Topoisomerase II complexes. This interaction disrupts the cleavage-relegation equilibrium of Topo II, resulting in formation of broken strands of DNA. Objective: To investigate the influence of type of substituents and substitution positions in 1,8- naphthalimde skeleton on the inhibition of Topoisomerase II activity. Methods: The starting 1,8-naphthalimide were prepared from acenaphthene by introduction of appropriate substituents followed by condensation with ω-hydroxylakylamines of different chain length. The substituents were introduced to 1,8-naphthalimide molecule by nucleophilic substitution of leaving groups like nitro or bromo present in 4 or 4,5- positions using the ω- hydroxylalkylamines. The bioactivity of obtained compounds was examined in model cell lines. Results: Antiproliferative activity of selected compounds against HCT 116 human colon cancer cells, human non-small cell lung cells A549 and non-tumorigenic BEAS-2B human bronchial epithelium cells was examined. Several of investigated compounds exhibit a significant activity (IC50 µM to 7 µM) against model cancer cell lines. It was demonstrated that upon treatment with concentration of 200 µM, all derivatives display Topo II inhibitory activity, which may be compared with activity of Amonafide. Conclusion: The replacement of the nitro groups in the chromophore slightly reduces its anticancer activities, whereas the presence of both nitro group and ω-hydroxylalkylamine chain resulted in seriously increased anticancer activity. Obtained compounds showed Topo II inhibitory activity, moreover, influence of the substitution pattern on the ability to inhibit Topo II activity and cancer cells proliferation was observed.

Inductive effect in EI-mass spectra of some 5,6-dihalogenides and 5,6-halohydrins of 5α-cholestan-3β-ol and 3β-acetoxy-5α-cholestane

1982 ◽  
Vol 47 (11) ◽  
pp. 2946-2960 ◽  
Author(s):  
Antonín Trka ◽  
Alexander Kasal
Keyword(s):  
Mass Spectra ◽  
Inductive Effect ◽  
Molecular Ions ◽  
Hydroxyl Group ◽  
Halogen Atoms ◽  
Derivatives Of

Partial EI-mass spectra of 3β-hydroxy- and 3β-acetoxy-5α-cholestanes substituted in positions 5α-, 6β- or 5α,6β- with a hydroxyl group or halogen atoms (fluorine, chlorine, bromine) are presented. The molecular ions of 5α,6β-disubstituted derivatives of 3β-hydroxy-5α-cholestane (or of its 3-acetate) are considerably more stable than the corresponding monosubstituted derivatives if at least one of the pair of the vicinal substituents is chlorine or fluorine. This increase in stability, most striking in 5α- and 6β-fluoro compounds, is explained by the inductive effect.

scholarly journals Increases of Lipophilic Antioxidants and Anticancer Activity of Coix Seed Fermented by Monascus purpureus

Foods ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 566
Author(s):  
Haiying Zeng ◽  
Likang Qin ◽  
Xiaoyan Liu ◽  
Song Miao
Keyword(s):  
Anticancer Activity ◽  
Radical Scavenging ◽  
Monascus Purpureus ◽  
Acid Oxidation ◽  
Anticancer Activities ◽  
Lipophilic Extract ◽  
Coix Seed ◽  
Before And After ◽  
Health Promoting ◽  
Human Laryngeal Carcinoma

Lipophilic tocols, γ-oryzanol, and coixenolide in coix seed before and after fermentation by Monascus purpureus were determined. Antioxidant and anticancer activities of raw and fermented coix seed were evaluated using free-radical-scavenging assays and polyunsaturated fatty acid oxidation model, and human laryngeal carcinoma cell HEp2, respectively. Compared to the raw seed, the tocols, γ-oryzanol, and coixenolide contents increased approximately 4, 25, and 2 times, respectively, in the fermented coix seed. Especially, γ-tocotrienol and γ-oryzanol reached 72.5 and 655.0 μg/g in the fermented coix seed. The lipophilic extract from fermented coix seed exhibited higher antioxidant activity in scavenging free radicals and inhibiting lipid oxidation. The inhibitory concentrations for 50% cell survival (IC50) of lipophilic extract from fermented coix seed in inhibiting HEp2 cells decreased by 42%. This study showed that coix seed fermented by M. purpureus increased free and readily bioavailable lipophilic antioxidants and anticancer activity. Therefore, fermentation could enhance the efficacy of the health promoting function of coix seeds.

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

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