Synthesis, Antiproliferative and Antioxidant Activity of 3-Mercapto-1,2,4-Triazole Derivatives as Combretastatin A-4 Analogues

Author(s):  
Sadiq Al-Mansury ◽  
Asim A. Balakit ◽  
Fatin Fadhel Alkazazz ◽  
Rana A. Ghaleb
2021 ◽  
Author(s):  
Yusuf SICAK

Abstract Due to the limited number of drugs in current clinical use, the diverse biological applications of furan have encouraged the preparation of a wide variety of thiosemicarbazide and triazole derivatives for the purpose of developing new drug agents. In this study aimed to investigate the antiproliferative and antioxidant activities of some thiosemicarbazides (1-12) and 1,2,4-triazoles (13-24). Compound 15 (IC50: 8.81±0.28 µM) showed the highest antiproliferative activity against the cervical (HeLa) cancer cell line among the compounds. Compounds 15, 20, 21, and 22 of the 1,2,4-triazole derivatives (13-24) exhibited excellent antioxidant activity. Moreover, the physicochemical properties, pharmacokinetic properties, drug similarity, and medicinal chemistry properties of all synthesized products were calculated using SwissADME. In addition, the effect of the structure–activity relationships of the 1,2,4-triazole derivatives (13-24) on the results of antiproliferative and antioxidant activity assays was evaluated.


2011 ◽  
Vol 44 (10) ◽  
pp. 525-527 ◽  
Author(s):  
T. V. Kochikyan ◽  
M. A. Samvelyan ◽  
E. V. Arutyunyan ◽  
V. S. Arutyunyan ◽  
A. A. Avetisyan ◽  
...  

2016 ◽  
Vol 148 (5) ◽  
pp. 917-923 ◽  
Author(s):  
Mahnaz Saraei ◽  
Zarrin Ghasemi ◽  
Gholamreza Dehghan ◽  
Marhamat Hormati ◽  
Khadijeh Ojaghi

2017 ◽  
Vol 87 (3-4) ◽  
pp. 191-200 ◽  
Author(s):  
Nidhal Soualeh ◽  
Aliçia Stiévenard ◽  
Elie Baudelaire ◽  
Rachid Soulimani ◽  
Jaouad Bouayed

Abstract. In this study, cytoprotective and antioxidant activities of Rosa canina (RC) and Salix alba (SA), medicinal plants, were studied on mouse primary splenocytes by comparing Controlled Differential Sieving process (CDSp), which is a novel green solvent-free process, versus a conventional technique, employing hydroethanolic extraction (HEE). Thus, preventive antioxidant activity of three plant powders of homogeneous particle sizes, 50–100 µm, 100–180 µm and 180–315 µm, dissolved directly in the cellular buffer, were compared to those of hydroethanolic (HE) extract, at 2 concentrations (250 and 500 µg/mL) in H2O2-treated spleen cells. Overall, compared to HE extract, the superfine powders, i. e., fractions < 180 µm, at the lowest concentration, resulted in greater reactive oxygen species (ROS) elimination, increased glutathione peroxidase (GPx) activity and lower malondialdehyde (MDA) production. Better antioxidant and preventive effects in pre-treated cells were found with the superfine powders for SA (i. e., 50–100 µm and 100–180 µm, both p < 0.001), and with the intermediate powder for RC (i. e., 100–180 µm, p < 0.05) versus HE extract. The activity levels of catalase (CAT) and superoxide dismutase (SOD) in pretreated splenocytes exposed to H2O2, albeit reduced, were near to those in unexposed cells, suggesting that pretreatment with the fine powders has relatively restored the normal levels of antioxidant-related enzymes. These findings supported that CDSp improved the biological activities of plants, avoiding the use of organic solvents and thus it could be a good alternative to conventional extraction techniques.


2021 ◽  
Vol 31 (1) ◽  
pp. 73-79
Author(s):  
Azalia Avila-Nava ◽  
Isabel Medina-Vera ◽  
Pamela Rodríguez-Hernández ◽  
Martha Guevara-Cruz ◽  
Pamela K. Heredia-G Canton ◽  
...  
Keyword(s):  

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
M Merlani ◽  
V Barbakadze ◽  
L Gogilashvili ◽  
L Amiranashvili ◽  
K Mulkijanyan ◽  
...  

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