Design and synthesis of novel benzimidazoles containing 1,2,3-triazolesas in vitro, anticancer and anti-oxidant agents

2021 ◽  
Vol 25 (11) ◽  
pp. 104-109
Author(s):  
Gullapelli Kumaraswamy ◽  
Ravichandar Maroju ◽  
Srinivas Bandari ◽  
Gouthami Dasari ◽  
Gullapelli Sadanandam

A novel series of 2-(1-((1-substitutedphenyl-1H-1,2,3- triazol-4-yl)methoxy)ethyl)-1-((1-substituted phenyl- 1H-1,2,3-triazol-4-yl)methyl)-1H-benzo[d]imidazole (3a-j)derivatives was synthesized in moderate to high yields. The structures of all the synthesized compounds were characterized by 1HNMR, 13CNMR and Mass spectroscopic methods. The title compounds were screened for their anti-oxidant activity and anti-cancer activity. The cancer activity results reveal that the compounds 3j, 3b and 3f are showing promising activity and remaining compounds exhibited moderate activity against all the tested cancer cell lines. The anti-oxidant activity also shows that the compounds 3c and 3d have shown excellent activity and remaining compounds were also found to exhibit moderate activity against the test organisms employed.

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (04) ◽  
pp. 61-69
Author(s):  
A. Rayaji ◽  
A. H. M. Viswanatha Swamy ◽  

Hepatocarcinogenesis is a multistep process involving different genetic alterations that ultimately lead to malignant transformation of the hepatocytes. Modern treatment of cancer includes chemotherapy, hormone therapy, radiotherapy and surgery but they are associated with several adverse effects such as alopecia, fatigue and general weakening of the body’s immune system due to bone marrow suppression. However, there is a continual need to look out for newer drugs to overcome the menace of cancer. In view of this we synthesized the new Coumarin-Cobalt complex derivatives. Structures of all the newly synthesized metal complexes are supported by Spectral data such as IR, NMR, and mass spectrometry. Coumarin-Cobalt complex of vanillin exhibited significant anti-cancer activity by in vivo anticancer activity (BrdU estimation). Immunohistochemical analysis has been done by BrdU and the synthesized compounds were screened for anti-oxidant activity and in vitro HepG2 cell lines. The IC50 values of the HepG2 cell lines as compared with that of standard Cisplatin and compounds IIIb, IIId, IIIe, IIIh and IIIj showed appreciable activity at a concentration less than 10 μG. Coumarin-Cobalt complex of vanillin exhibited significant anti-cancer activity. Anti-oxidant activity performed by Nitric oxide reducing ability, Superoxide dismutase and reducing activity:Compounds IIIc, IIIe and IIIg showed appreciable activity at 400μg/mL and 800 μg/mL screened by nitric oxide reducing ability, superoxide anion was effectively scavenged by compound IIIg at 400μg/mL and 800 μg/mL and reducing power of compounds IIIc and IIIj is comparable with standard ascorbic acid at concentrations 400μg/mL and 800 μg/mL.


2020 ◽  
Author(s):  
Liang Qi ◽  
Linxia Xiao ◽  
Rui Lin

An efficient and metal free methodology for the synthesis of bis(indolyl)methanes (BIMs) and bis(aryl)alkanes derivatives in the presence of B(C6F5)3 by the condensation of primary amines with pyruvates with good to high yields have been successfully developed. Some BIMs derivatives displayed good in vitro antitumor activity, screened by MTT assay. Compound 3b show the best anti-cancer activity against lung carcinoma cell A549 cells with IC50 of 4.52 µM.


2013 ◽  
Vol 16 (20) ◽  
pp. 1212-1215 ◽  
Author(s):  
Mohammadjavad Paydar ◽  
Yi Li Wong ◽  
Bushra Abdulkarim Moharam ◽  
Won Fen Wong ◽  
Chung Yeng Looi

2018 ◽  
Vol Volume-2 (Issue-4) ◽  
pp. 289-292
Author(s):  
Dinesh M. D ◽  
Neethu George ◽  
Abdul Bari. K. K | Hima K. U | S. Meenatchisundaram ◽  

2019 ◽  
Vol 16 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Mohammed Abdul Mujeeb ◽  
Ankalabasappa Vedamurthy ◽  
Arun Kashivishwanath Shettar ◽  
Sridevi Indrajeet Puranik ◽  
Shridhar Ghagane ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4424
Author(s):  
Uzma Arshad ◽  
Sibtain Ahmed ◽  
Nusrat Shafiq ◽  
Zaheer Ahmad ◽  
Aqsa Hassan ◽  
...  

Objective: In this study, small molecules possessing tetrahydropyrimidine derivatives have been synthesized having halogenated benzyl derivatives and carboxylate linkage. As previously reported, FDA approved halogenated pyrimidine derivatives prompted us to synthesize novel compounds in order to evaluate their biological potential. Methodology: Eight pyrimidine derivatives have been synthesized from ethyl acetoacetate, secondary amine, aromatic benzaldehyde by adding catalytic amount of CuCl2·2H2O via solvent less Grindstone multicomponent reagent method. Molecular structure reactivity and virtual screening were performed to check their biological efficacy as an anti-oxidant, anti-cancer and anti-diabetic agent. These studies were supported by in vitro analysis and QSAR studies. Results: After combined experimental and virtual screening 5c, 5g and 5e could serve as lead compounds, having low IC50 and high binding affinity.


Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4265
Author(s):  
Victor Carramiñana ◽  
Ana M. Ochoa de Ochoa de Retana ◽  
Francisco Palacios ◽  
Jesús M. de los de los Santos

Several phosphorus-substituted N-acylated cyanoaziridines 2 and N-carbamoylated cyanoziridines 5 were prepared in good to high yields. N-Acylated cyanoaziridines 2 were used, after ring expansion, in an efficient synthesis of oxazoline derivative 3a and in a completely regio-controlled reaction in the presence of NaI. Conversely, N-carbamoyl cyanoaziridines 5 reacted with NaI to obtain a regioisomeric mixture of 2-aminocyanooxazolines 7. Mild acidic conditions can be used for the isomerization of N-thiocarbamoyl cyanoaziridine 6a into a 2-aminocyanothiazoline derivative 8a by using BF3·OEt2 as a Lewis acid. Likewise, a one pot reaction of NH-cyanoaziridines 1 with isocyanates obtained 2-iminocyanooxazolidines 9 regioselectively. This synthetic methodology involves the addition of isocyanates to starting cyanoaziridines to obtain N-carbamoyl cyanoaziridines 5, which after the ring opening, reacts with a second equivalent of isocyanate to give the final 2-imino cyanooxazolidines 9. In addition, the cytotoxic effect on the cell lines derived from human lung adenocarcinoma (A549) was also screened. 2-Iminooxazolidines 9 exhibited moderate activity against the A549 cell line in vitro. Furthermore, a selectivity towards cancer cells (A549) over non-malignant cells (MCR-5) was detected.


RSC Advances ◽  
2017 ◽  
Vol 7 (6) ◽  
pp. 3408-3412 ◽  
Author(s):  
Long Ma ◽  
Haiyan Liu ◽  
Lingpei Meng ◽  
Ping Qin ◽  
Botao Zhang ◽  
...  

Triterpenoidal saponins fraction isolated from a traditional Chinese medicine Conyza blinii H. Lév. demonstrates anti-cancer activity both in vitro and in vivo.


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