Researches on the Synthesis and Biological Activity of 1,2,4-tiadizoles-3,5-disubstituted using Ditiazolium Salts as Precursors

2008 ◽  
Vol 59 (1) ◽  
pp. 101-105
Author(s):  
Irina Zarafu ◽  
Lucia Veronica Ivan ◽  
Iuliana Harasim

3,5-disubstituted-1,2,4-tiadiazoles with substituted-styril and heterocycle-vinyl were obtained by extending the method which implies the use of 3,5-disubstituted-1,2,4-ditiazolium salts as precursors [1-4]. A comparative study of the reaction process in the case of perchlorates, diacide phosphates, tribromides and 3,5-distyrile-dithiazolium triiodides, taken as etalon, was perfomed. Good yields were obtained when using perchlorates, phosphates and triiodides. The reaction was made by heating the reaction mixture and by ultrasound exposure. The structure of the compounds was confirmed by chemical and physical analysis and the data obtained were identical to those of 3,5-disubstituted-1,2,4-tiadiazoles obtained by another methods [5,6]. The biological (antibacterial and anticancer) activity of the synthesized compounds was tested and the results indicated a medium activity.

3 Biotech ◽  
2021 ◽  
Vol 11 (2) ◽  
Author(s):  
S. C. Esparza González ◽  
Ena Bolaina-Lorenzo ◽  
J. J. Pérez-Trujillo ◽  
B. A. Puente-Urbina ◽  
O. Rodríguez-Fernández ◽  
...  

2020 ◽  
Vol 20 (19) ◽  
pp. 2019-2035
Author(s):  
Esmaeil Sheikh Ahmadi ◽  
Amir Tajbakhsh ◽  
Milad Iranshahy ◽  
Javad Asili ◽  
Nadine Kretschmer ◽  
...  

Naturally occurring naphthoquinones (NQs) comprising highly reactive small molecules are the subject of increasing attention due to their promising biological activities such as antioxidant, antimicrobial, apoptosis-inducing activities, and especially anticancer activity. Lapachol, lapachone, and napabucasin belong to the NQs and are in phase II clinical trials for the treatment of many cancers. This review aims to provide a comprehensive and updated overview on the biological activities of several new NQs isolated from different species of plants reported from January 2013 to January 2020, their potential therapeutic applications and their clinical significance.


2018 ◽  
Vol 18 (5) ◽  
pp. 739-746 ◽  
Author(s):  
Raj Kaushal ◽  
Nitesh Kumar ◽  
Archana Thakur ◽  
Kiran Nehra ◽  
Pamita Awasthi ◽  
...  

Abstract: Background: After the discovery of cisplatin, first non platinum anticancer drugs having excellent efficacy were budotitane and TiCl2(cp)2 but action mechanism is not clear. Therefore, we hereby reporting synthesis and biological activities novel titanium complexes to explore their mode of action. Objectives: Synthesis, spectral characterization, antibacterial and anticancer activity of some titanium complexes. Antibacterial studies on various bacterial strains and anticancer studies on HeLa, C6, CHO cancerous cell lines have been performed. Further, the cell death mechanistic study was done on CHO cell lines. Method: Titanium complexes with and without labile groups have been synthesized by reacting of TiCl4 with nitrogen containing ligands viz. 1,2-diaminocyclohexane, 1,10-Phenanthroline, adamantylamine, 2,2'-bipyridine, 4,4'-dimethyl-2,2'-bipyridine in predetermined molar ratios. Antibacterial and anticancer studies were performed by agar well diffusion method and MTT assay respectively. Cell cycle analysis is done by using flow cytometry. Results: Complex 2 i.e TiCl2(Phen)2 showed better activity than other complexes as an antibacterial as well as anticancer agent. Phase contrast imaging indicates that observed morphological changes of cells was dose dependent. Cell death mechanistic study have shown the increase in sub G0 phase population as well as formation of blebbing and fragmentation of chromatin material which is an indicative measure of apoptosis. Conclusion: Complex 2 proved to be more effective bactericide and cytotoxic agent. Cell cycle analysis showed cell arrest in G0 phase. Apoptosis percentage was found to increase in a dose dependent manner. So, prepared titanium complexes can be put to use as an important chemotherapeutic agents.


Nanomedicine ◽  
2019 ◽  
Vol 14 (9) ◽  
pp. 1173-1189 ◽  
Author(s):  
Bhuban Ruidas ◽  
Sutapa Som Chaudhury ◽  
Kunal Pal ◽  
Prashanta Kumar Sarkar ◽  
Chitrangada Das Mukhopadhyay

2021 ◽  
Vol 26 (3) ◽  
pp. 100-108
Author(s):  
Ahmed Mouard ◽  
Hassan Mesbah ◽  
Rehab AlAssar ◽  
Khaled Abd ElHamid

2018 ◽  
Vol 41 (2) ◽  
Author(s):  
Ramasubba Reddy Palem ◽  
Shimoga D Ganesh ◽  
Zuzana Kronekova ◽  
Monika Sláviková ◽  
Nabanita Saha ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3604 ◽  
Author(s):  
Sijongesonke Peter ◽  
Blessing Atim Aderibigbe

Malaria and cancer are chronic diseases. The challenge with drugs available for the treatment of these diseases is drug toxicity and resistance. Ferrocene is a potent organometallic which have been hybridized with other compounds resulting in compounds with enhanced biological activity such as antimalarial and anticancer. Drugs such as ferroquine were developed from ferrocene and chloroquine. It was tested in the 1990s as an antimalarial and is still an effective antimalarial. Many researchers have reported ferrocene compounds as potent compounds useful as anticancer and antimalarial agents when hybridized with other pharmaceutical scaffolds. This review will be focused on compounds with ferrocene moieties that exhibit either an anticancer or antimalarial activity.


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