scholarly journals A Novel Series of Thiazoles and 1,3,4-Thiadiazoles Bearing Thiazole Moiety as Anticancer Agents: Synthesis, Spectral Studies, Biological Evaluation and Structure Activity relationship

2016 ◽  
Author(s):  
Sobhi M. Gomha ◽  
Nabila A. Kheder ◽  
Mohamad R. Abdelaziz ◽  
Yahia Nasser Mabkhot
Keyword(s):  
Cell Line ◽  
Carcinoma Cell ◽  
Structure Activity Relationship ◽  
Biological Evaluation ◽  
Carcinoma Cell Line ◽  
Activity Relationship ◽  
Spectral Studies ◽  
Liver Carcinoma ◽  
Structure Activity ◽  
Carcinoma Cell Line Hepg2

A novel series of thiazole based-1,3,4-thiadiazoles were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbothioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were established based on spectroscopic evidences and their alternative syntheses. Thirteen new 1,3,4-thiadiazoles have been evaluated for their anticancer activity against liver carcinoma cell line (HepG2). Also, their structure activity relationship (SAR) was studied. The 1,3,4-thiadiazoles 12d, 12c, 6g,18b, 6c, and 6f(IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) have promising antitumor activity against liver carcinoma cell line (HepG2).

scholarly journals Synthesis and biological evaluation of new aryl substituted Schiff’s bases

2017 ◽  
Vol 4 (6) ◽  
pp. 252
Author(s):  
Versha Parcha ◽  
Jaswinder Kaur
Keyword(s):  
Antimicrobial Agents ◽  
Acid Hydrazide ◽  
Structure Activity Relationship ◽  
Biological Evaluation ◽  
Activity Relationship ◽  
Spectral Studies ◽  
Schiff’S Bases ◽  
Structure Activity ◽  
Schiff's Bases ◽  
Good Potential

Objective: Chemical substances employed to treat various infections caused by various types of microorganism are termed as antimicrobials and natural chemical compounds produced by specific types of bacteria are termed as antibiotics. Unlimited use of antibiotics in humans and animals and in areas other than the treatment and prophylaxis of disease have resulted in a serious problem of drug resistance. Various attempts have been adopted to cope with the resistance problem and enhance the activity, or broaden the spectrum of drugs. Based on structure-activity relationship synthesis of new compounds has been one of the best approaches for better results. It has been demonstrated that Schiff base of some leading molecules and antibiotics possess good potential as more effective and safe drugs. Encouraged by reports on potential of Schiff’s bases as antimicrobial agents and to cope up with the current requirements of developing newer, safer and broad spectrum agents attempts were made to synthesize new Schiff’s bases.Methods: Our earlier in which structure activity relationship studies revealed that substitution by nitro and amino gp in Schiff’s base moiety resulted in the enhancement of activity. So further attempts were made to extend the series with incorporation of nitro and amino moiety by condensing o,m dinitro substituted acid hydrazide with various nitro/amino substituted benzaldehydes for increasing their antimicrobial potential.Results: Synthesized compounds were characterized on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect. All the synthesized derivatives were screened further for their antibacterial effect.Conclusions: Highest activity was observed in the derivative with nitro substitution in both the aryl rings.

scholarly journals Cytotoxic Effects of Hydro-Alcoholic Extract of the Leaf of Elaeagnus angustifolia in Hepatocellular Carcinoma Cell Line (HepG2)

2020 ◽  
Vol 11 (3) ◽  
Author(s):  
Manijeh Ghanghareh ◽  
Maryam Zare
Keyword(s):  
Side Effects ◽  
Redox Potential ◽  
Cell Line ◽  
Hepg2 Cells ◽  
Carcinoma Cell ◽  
Carcinoma Cell Line ◽  
New Drugs ◽  
Liver Carcinoma ◽  
Alcoholic Extract ◽  
Carcinoma Cell Line Hepg2

Background: Cancer is one of the most complicated diseases with various treatments, which each has its special side effects. So, pharmaceutical companies are intended to develop new drugs with minimum side effects. Objectives: The current study aimed to investigate the cytotoxicity effects and the redox potential of alcoholic extract of Oleaster leaf on liver carcinoma cell line (HepG2). Methods: Oleaster leaves were collected from Qazvin (Iran), and the alcoholic extract of the plant leaves was prepared. HepG2 cells were cultured in DMEM medium and treated with 50, 100, 200, 400, and 600 μg/mL of the extract. The cytotoxicity effect of the extract was evaluated using the MTT and the Neutral Red assays. Redox potential in HepG2 cells was assessed using NO, catalase, and GSH tests. The expression of Bax and bcl-2 genes in HepG2 cells was evaluated for apoptosis analysis. Results: The results showed that the extract could significantly (P < 0.001) reduce the viability of HepG2 cells. Also, the extract significantly increased the amount of released NO, catalase activity, and GSH concentration. RT-PCR results showed that Oleaster leaf extract significantly change the expression of bax and bcl-2. Conclusions: The results showed that the leaves of the Oleaster plant contain compounds with cytotoxicity properties, so it can be considered as a potent candidate for liver cancer treatment.

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