Synthesis and Antioxidant Activity of New N-Containing Hybrid Derivatives of Gallic and Ursolic Acids

2021 ◽  
Author(s):  
S. A. Popov ◽  
C. Wang ◽  
Z. Qi ◽  
E. E. Shul’ts ◽  
M. Turks
Keyword(s):  
Antioxidant Activity ◽  
Derivatives Of

Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

Antioxidant activity of some derivatives of 9-thiabicyclo[3,3,1]nonane in rubber and rubber vulcanizates

1992 ◽  
Vol 37 (1) ◽  
pp. 1-5 ◽  
Author(s):  
J.-M. Herdan ◽  
Liana Cira ◽  
Maria Giurginca ◽  
G. Ivan
Keyword(s):  
Antioxidant Activity ◽  
Derivatives Of

Two in one: bifunctional derivatives of trolox acting as antimalarial and antioxidant agents

2020 ◽  
Vol 12 (20) ◽  
pp. 1845-1854
Author(s):  
Florence Souard ◽  
Edwige Nicolle ◽  
Delphine Cressend ◽  
Alexis Valentin ◽  
Ahcène Boumendjel
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
In Vivo Studies ◽  
Chemical Libraries ◽  
Falciparum Strain ◽  
Antioxidant Agents ◽  
One Step ◽  
Set Up ◽  
Derivatives Of

Background: The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results: Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion: Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.

scholarly journals Synthesis, Antimicrobial and Antioxidant Activities of 2-Isoxazoline Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4271
Author(s):  
Asma Alshamari ◽  
Mahmoud Al-Qudah ◽  
Fedaa Hamadeh ◽  
Lo’ay Al-Momani ◽  
Sultan Abu-Orabi
Keyword(s):  
Antioxidant Activity ◽  
Sulfonic Acid ◽  
Antioxidant Activities ◽  
Bacterial Species ◽  
Antibacterial Activities ◽  
Ms Analysis ◽  
Diammonium Salt ◽  
New Compounds ◽  
Derivatives Of

A series of derivatives of trans-3-(2,4,6-trimethoxyphenyl)4,5-dihydroisoxazolo-4,5-bis[carbonyl-(4′phenyl)thiosemicarbazide (9) and of trans-3-(2,4,6-trimethoxyphenyl)-4,5-dihydro isoxazolo-4,5-bis(aroylcarbohydrazide) (10a–c) were synthesized from trans-3-(2,4,6-trimethoxyphenyl)-4,5-dihydro-4,5-bis(hydrazenocarbonyl)isoxazole (8). The structures of the compounds were elucidated by both elemental and spectral (IR, NMR, and MS) analysis. Compound 9 shows activity against some bacterial species. No antibacterial activities were observed for compounds 10a–c. The antioxidant activity of the new compounds has been screened. Compound 9 showed higher antioxidant activity using the DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2’-azino–bis(3-ethylbenzoline-6-sulfonic acid) diammonium salt methods.

ChemInform Abstract: Synthesis of Novel Biaryl Derivatives of Sesamol (5-Benzodioxolol) and Evaluation of Their Antioxidant Activity Against DPPH Radical.

ChemInform ◽  
2014 ◽  
Vol 45 (14) ◽  
pp. no-no
Author(s):  
Sergio A. Rodriguez ◽  
Monica A. Nazareno ◽  
Maria T. Baumgartner
Keyword(s):  
Antioxidant Activity ◽  
Dpph Radical ◽  
Derivatives Of

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.

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