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.

scholarly journals Sintesis Dan Uji Aktivitas Antioksidan Senyawa Flavonol 2-(3,4,5-Dimetoksifenil)-3-Hidroksi-4h-Kromen-4-On

2019 ◽  
Vol 2 (2) ◽  
pp. 34-37
Author(s):  
Muhamad Rokhim ◽  
Adel Zamri ◽  
Hilwan Yuda Teruna
Keyword(s):  
Antioxidant Activity ◽  
Spectroscopic Data ◽  
Dpph Assay ◽  
Ic50 Values ◽  
Derivatives Of

Flavonols 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 HPLC, UV, FTIR, NMR and HRMS. Antioxidant activity was evaluated using the DPPH assay which showed that the flavonol 2'-hydroxycalone derivative was potentially active as antioxidants with IC50 values <1000 µg / mL.

scholarly journals Antioxidant and Anticancer Activity of Novel Derivatives of 3-[(4-Methoxyphenyl)amino]propanehydrazide

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 2980 ◽  
Author(s):  
Ingrida Tumosienė ◽  
Kristina Kantminienė ◽  
Arnas Klevinskas ◽  
Vilma Petrikaitė ◽  
Ilona Jonuškienė ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Triple Negative ◽  
Radical Scavenging ◽  
13C Nmr Spectroscopy ◽  
Molecular Structures ◽  
Mass Spectrometry Data ◽  
Derivatives Of ◽  
Dpph Radical Scavenging

Series of novel 3-[(4-methoxyphenyl)amino]propanehydrazide derivatives bearing semicarbazide, thiosemicarbazide, thiadiazole, triazolone, triazolethione, thiophenyltriazole, furan, thiophene, naphthalene, pyrrole, isoindoline-1,3-dione, oxindole, etc. moieties were synthesized and their molecular structures were confirmed by IR, 1H-, 13C-NMR spectroscopy and mass spectrometry data. The antioxidant activity of the synthesized compounds was screened by DPPH radical scavenging method. The antioxidant activity of N-(1,3-dioxoisoindolin-2-yl)-3-((4-methoxyphenyl)amino)propanamide and 3-((4-methoxyphenyl)amino)-N’-(1-(naphthalen-1-yl)-ethylidene)propanehydrazide has been tested to be ca. 1.4 times higher than that of a well-known antioxidant ascorbic acid. Anticancer activity was tested by MTT assay against human glioblastoma U-87 and triple-negative breast cancer MDA-MB-231 cell lines. In general, the tested compounds were more cytotoxic against U-87 than MDA-MB-231 cell line. 1-(4-Fluorophenyl)-2-((5-(2-((4-methoxyphenyl)amino)ethyl)-4-phenyl-4H-1,2,4-triazol-3-yl)thio)ethanone has been identified as the most active compound against the glioblastoma U-87 cell line.

scholarly journals Amino- and polyaminophthalazin-1(2H)-ones: synthesis, coordination properties, and biological activity

2021 ◽  
Vol 17 ◽  
pp. 558-568
Author(s):  
Zbigniew Malinowski ◽  
Emilia Fornal ◽  
Agata Sumara ◽  
Renata Kontek ◽  
Karol Bukowski ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metal Ion ◽  
Spectroscopic Data ◽  
Anticancer Activities ◽  
Biological Screening ◽  
Biological Assays ◽  
Palladium Catalyzed ◽  
Amino Derivatives ◽  
Derivatives Of ◽  
Ht 29

Amino- and polyaminophthalazinones were synthesized by the palladium‐catalyzed amination (alkyl- and arylamines, polyamines) of 4-bromophthalazinones in good yields. The coordinating properties of selected aminophthalazinones towards Cu(II) ions were investigated and the participation of the nitrogen atoms in the complexation of the metal ion was shown. A biological screening of the potential cytotoxicity of selected synthesized compounds on HT-29 and PC-3 cell lines, as well as on the L-929 cell line, proved that some amino derivatives of phthalazinone show interesting anticancer activities. The detailed synthesis, spectroscopic data, and biological assays are reported.

scholarly journals Secondary Metabolites with α-Glucosidase Inhibitory Activity from the Mangrove Fungus Mycosphaerella sp. SYSU-DZG01

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 483 ◽  
Author(s):  
Pei Qiu ◽  
Zhaoming Liu ◽  
Yan Chen ◽  
Runlin Cai ◽  
Guangying Chen ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Secondary Metabolites ◽  
Single Crystal ◽  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
X Ray Diffraction ◽  
X Ray ◽  
Ic50 Values ◽  
New Metabolites

Four new metabolites, asperchalasine I (1), dibefurin B (2) and two epicoccine derivatives (3 and 4), together with seven known compounds (5–11) were isolated from a mangrove fungus Mycosphaerella sp. SYSU-DZG01. The structures of compounds 1–4 were established from extensive spectroscopic data and HRESIMS analysis. The absolute configuration of 1 was deduced by comparison of ECD data with that of a known structure. The stereostructures of 2–4 were further confirmed by single-crystal X-ray diffraction. Compounds 1, 8 and 9 exhibited significant α-glucosidase inhibitory activity with IC50 values of 17.1, 26.7 and 15.7 μM, respectively. Compounds 1, 4, 6 and 8 showed antioxidant activity by scavenging DPPH· with EC50 values ranging from 16.3 to 85.8 μM.

scholarly journals Anticancer Activity, Antioxidant Activity, and Phenolic and Flavonoids Content of Wild Tragopogon porrifolius Plant Extracts

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Fuad Al-Rimawi ◽  
Suzi Rishmawi ◽  
Sharehan H. Ariqat ◽  
Mahmoud F. Khalid ◽  
Ismail Warad ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Plant Extracts ◽  
Folk Medicine ◽  
Reducing Power ◽  
Total Phenolic ◽  
Osteosarcoma Cell ◽  
Anticancer Activities ◽  
Antioxidant Power

Tragopogon porrifolius, commonly referred to as white salsify, is an edible herb used in folk medicine to treat cancer. Samples of Tragopogon porrifolius plant grown wild in Palestine were extracted with different solvents: water, 80% ethanol, and 100% ethanol. The extracts were analyzed for their total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity (AA). Four different antioxidant assays were used to evaluate AA of the extracts: two measures the reducing power of the extracts (ferric reducing antioxidant power (FRAP) and cupric reducing antioxidant power (CUPRAC)), while two other assays measure the scavenging ability of the extracts (2,2-azino-di-(3-ethylbenzothialozine-sulphonic acid (ABTS)) and 2,2-diphenyl-1-picrylhydrazyl (DPPH)). Anticancer activity of the plant extracts were also tested on HOS and KHOS osteosarcoma cell lines. The results revealed that the polarity of the extraction solvent affects the TPC, TFC, and AA. It was found that both TPC and AA are highest for plant extracted with 80% ethanol, followed by water, and finally with 100% ethanol. TFC however was the highest in the following order: 80% ethanol > 100% ethanol > water. The plant extracts showed anticancer activities against KHOS cancer cell lines; they reduced total cell count and induced cell death in a drastic manner.

Telomere DNA Binding, Cleavage and Anticancer Activity of [Cu(phendione)(Hpyramol)Cl]

2019 ◽  
Vol 13 (2) ◽  
pp. 171-182
Author(s):  
Palanisamy Uma Maheswari ◽  
Renuga Duraisamy ◽  
Murugesan Kanagavel ◽  
Kalimuthusamy Natarajaseenivasan ◽  
Kadhar Mohamed Meera Sheriffa Begum ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Dna Cleavage ◽  
Phenoxyl Radical ◽  
Anticancer Activities ◽  
Redox Active ◽  
G Quadruplex ◽  
Ic50 Values ◽  
Controlled Potential ◽  
Human Telomere

Background:The ligand Hpyramol is a redox active, which on coordination with Cu(II) cleaves DNA without any added reductant. Another ligand phendione is known for its wide application towards anticancer activities. We combined the ligands with CuCl2 to have an intercalation moiety and a redox active ligand in participation towards telomere DNA cleavage and anticancer activity.Objective:In this study, our aim is to interact it with Human telomere DNA and to see their effects on cancer cells.Methods:The complex [Cu(L)(L’)Cl] has interacted with the human telomere DNA sequence (TTAGGG), HTelo20. The HTelo20 was stabilized under both parallel and antiparallel G-quadruplex conformations and the complex [Cu(L)(L’)Cl] has interacted followed by circular dichroism spectroscopy and gel electrophoresis.Results:The parallel G-quadruplex and randomly coiled conformations of HTelo20 were easily cleaved than the anti-parallel G-quadruplex conformation. The nature of DNA cleavage was found to be oxidative rather hydrolytic. The formation of phenoxyl radical species under electrochemical and controlled potential electrolysis conditions by the complex [Cu(L)(L’)Cl] proves the possibility of oxidative nature of DNA cleavage. The comet assay also proves the DNA cleavage induced by the complex [Cu(L)(L’)Cl] inside the nucleus of HeLa cancer cells.Conclusion:The complex [Cu(L)(L’)Cl] was tested for anticancer activity, induced by ROS and DNA cleavage. The IC50 values resulted in nanomolar concentrations with selected cancer cell lines. Relatively the Cu complex shows less toxicity with the normal cell line L132.

scholarly journals Thiazolidinedione or Rhodanine: A Study on Synthesis and Anticancer Activity Comparison of Novel Thiazole Derivatives

2017 ◽  
Vol 20 (1) ◽  
pp. 415 ◽  
Author(s):  
Cigdem Ozen ◽  
Meltem Ceylan Unlusoy ◽  
Nazanin Aliary ◽  
Mehmet Ozturk ◽  
Oya Bozdag Dundar
Keyword(s):  
Hepatocellular Carcinoma ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Condensation Reaction ◽  
Huh7 Cell ◽  
Anticancer Activities ◽  
Thiazole Derivatives ◽  
Ic50 Values ◽  
Huh7 Cell Line

Purpose: A new series of thiazolyl-2,4-thiazolidinedione / rhodanine compounds T1-T23 was synthesized and tested for their anticancer activities. Hepatocellular carcinoma cell lines were chosen due to their strong drug resistance to test the new compounds. Methods: All compounds were synthesized via Knoevenagel Condensation reaction and thiazolidinedione ester compounds (T3,T9,T15,T20) were hydrolyzed for obtaining the acidic compounds (T6,T12,T17,T23). All compounds were firstly screened for their anticancer activity against two hepatocellular carcinoma (HCC) cell lines, Huh7 and Plc/Prf/5 (Plc) cell lines by sulforhodamine B assay. Further IC50 values were calculated for three candidates (T4, T15, T21) in five different HCC (Huh7, Plc, Snu449, HepG2, Hep3B) and one breast cancer (Mcf7) cell line. Results: Compounds T4, T15, T21 had very strong anticancer effects even though their 10 µM concentration in Huh7 cell line. According to IC50 values, T21 was the most effective compound with IC50 values in a range from 2 to 16 µM in 6 cancer cell lines. In terms of cytotoxicity T21 mostly affected Huh7 and interestingly it was less effective against Plc. Conclusions: Considering these results it can be suggested that compounds T4, T15 and T21 may lead to the development of more potent anticancer drugs in the future. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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...

Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohan H. Patil ◽  
Uma D. Kabra ◽  
Krishna R. Gupta ◽  
Milind J. Umekar
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

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