scholarly journals Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Abdulrhman Alsayari ◽  
Yahya I. Asiri ◽  
Abdullatif Bin Muhsinah ◽  
Mohd. Zaheen Hassan

Background. Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. Methods. The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. Results. One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). Conclusion. In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents.

2019 ◽  
Vol 31 (3) ◽  
pp. 744-750 ◽  
Author(s):  
Sara Nabil ◽  
Abeer Obaid Al-Dossary

A series of novel pyridazine, pyrazoles, pyrimidines derivatives have been synthesized through the reaction of chloropyridazine (1) with p-phenylenediamine to give compound 2. Diazotization of compound 2 followed by coupling with active methylene compounds namely acetylacetone, ethylcyanoacetate and/or ethylacetoacetate afforded novel hydrazons derivatives (4-6). The resulting hydrazons can have been cyclized using hydrazine hydrate and guanidine gave the corresponding pyrazoles (7-9) and pyimidine (10) derivatives. Reaction of compound 2 with acrylonitrile, aromatic aldehyde, p-chloroacetophenone and phenyl isothiocyanate gave compounds 11, 12a, 12b, 13 and 17, respectively. The latter compounds have been used in synthesis of some heterocyclic compounds. The cytotoxic activity of the most active compounds was assessed in vitro against breast carcinoma cell line (MCF-7), human liver cancer cell line (HEPG2), human colon cancer cell line (HCT). Compounds 4, 8 showed best activity against MCF-7 cell line, compounds 5, 13a showed best activity against HePG2 cell line and compound 10 showed best activity against HCT cell line.


2020 ◽  
Vol 16 (4) ◽  
pp. 419-431
Author(s):  
Kishore K. Valluri ◽  
Tejeswara R. Allaka ◽  
IV Kasi Viswanath ◽  
Nagaraju PVVS

Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of novel scaffolds are described by variation in therapeutic effects of parent molecule. The structure variants were characterized by using a blend of spectroscopic 1H NMR, 13C NMR, IR, Mass and chromatographic techniques. Results: When tested for in vitro antibacterial and anticancer activities, several of these compounds showed good activities. The target compounds 9b, 9a and 9e exhibited a high degree of anticancer activity against human colon cancer cell line Caco-2 and human breast cancer cell line MDAMB231. Further, 9a, 9b, 9d, and 9h showed better activity towards four medically relevant organisms; Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Klebsiella Species compared to CPF. In the present investigation, cheminfomatics tools Molinspiration, 2003 and MolSoft, 2007 for the prediction of insilico molecular properties and drug likeness for the target compounds 9a-h was evaluated and positive results were observed. Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antibacterial/ anticancer agents.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.


Oncogene ◽  
2001 ◽  
Vol 20 (35) ◽  
pp. 4884-4890 ◽  
Author(s):  
Duyen T Dang ◽  
Channing S Mahatan ◽  
Long H Dang ◽  
Iyabode A Agboola ◽  
Vincent W Yang

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