scholarly journals Synthesis, Characterization and Cytotoxic Activity of some new 1,2,3-Triazole, Oxadiazole and Aza- β-lactam Derivatives

2018 ◽  
Vol 34 (5) ◽  
pp. 2350-2360 ◽  
Author(s):  
Kany A. Abdulqader ◽  
Ahmed W. Naser ◽  
Muthanna S. Farhan ◽  
Sabah J. Salih
Keyword(s):  
Cytotoxic Activity ◽  
Schiff Bases ◽  
Click Reaction ◽  
Phenyl Isocyanate ◽  
Consecutive Reaction ◽  
Cytotoxic Effects ◽  
Cellular Models ◽  
Mcf7 Cell Line ◽  
Benzamide Derivatives ◽  
Previous Reaction

A series of 1,2,3-triazole, oxadiazole and aza-β-lactam derivatives were synthesized through consecutive reaction began from o-(N-propargyl) sulfonamido benzoic acid (1a). The reaction of (1a) with absolute ethanol in the presence of concentrated H2SO4 resulted in the formation of ester derivative (2a). The product of the previous reaction was reacted with 80% hydrazine hydrate to prepare benzohydrazide derivative (3a). 1,3,4-oxadiazole compound (4a) was obtained by condensation of compound (3a) with CS2 in presence KOH . Compound (3a) react with Phenyl isocyanates to give Carboxamide derivative (5a), that Condensation either with 2,4-dimethoxybenzaldhyde and p-hydroxybenzaldehyde to prepare the Schiff bases (6a-b). The cycloaddotion of Schiff-bases (6a-b) with phenyl isocyanate gave aza-β-lactams (7a-b). Benzamide derivatives (8a-c) were prepared via the reaction of compound (1a) with aniline derivatives, such as (p-toluidine, o-nitroaniline and m-nitroaniline). In a regioselective reaction 1,4-disubstituted-1,2,3-triazole derivative (9a-j) were synthesized via the click reaction of compounds 4a,5a and (8a-c) with benzyl azide and p-bromobenzyl azide. The compounds were identified using the spectral methods shown in the work. Cytotoxic effects of some final prepared compounds were studied in one cultured cellular models (MCF7 cell line) breast cancer (at various concentrations) by MTT assay, compound (9j) showed the better cytotoxic activity among the tested compounds.

ChemInform Abstract: Novel Sesquiterpenes from Schisandra grandiflora: Isolation, Cytotoxic Activity and Synthesis of Their Triazole Derivatives Using “click” Reaction.

ChemInform ◽  
2015 ◽  
Vol 46 (26) ◽  
pp. no-no
Author(s):  
B. Poornima ◽  
Bandi Siva ◽  
G. Shankaraiah ◽  
A. Venkanna ◽  
V. Lakshma Nayak ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Click Reaction ◽  
Triazole Derivatives

Eryngium billardieri Extract and Fractions Induces Apoptosis in Cancerous Cells

2021 ◽  
Vol 21 ◽  
Author(s):  
Samira Hasanbeiglu ◽  
Kamran Hosseini ◽  
Ommoleila Molavi ◽  
Parina Asgharian ◽  
Vahideh Tarhriz
Keyword(s):  
Cell Lines ◽  
Mcf7 Cell ◽  
Inhibitory Effect ◽  
P Value ◽  
Breast Cancers ◽  
Natural Habitats ◽  
Cytotoxic Effects ◽  
Soxhlet Apparatus ◽  
Mcf7 Cell Line ◽  
Cancerous Cells

Background: Eryngium is genus flowering plants in the Umbelliferae family having pharmacological properties such as anti-inflammatory and anti-diabetic. Given the nature of melanoma and breast cancers in recent years and the fact that the anti-cancer properties of Eryngium billardieri on mentioned cell lines have not been studied, the present study conducted to explore these properties. Objective: The mechanisms of cytotoxicity and apoptosis of aerial parts of various extracts and fractions of E. billardieri on cancerous cells and normal cells were investigated. Methods: Samples were collected from natural habitats, dried and then extracted by Soxhlet apparatus with solvents of n-Hex, DCM and methanol, respectively. The cytotoxic effects of the extracts were investigated by MTT method on MCF7, B16 and HFF-2 classes for 24 and 48 hours. Flowcytometry, was also used to investigate the mechanism of cytotoxicity and confirming by Real-time PCR of p53 and Bax genes, which codes apoptosis regulator proteins. Meanwhile, volatile compounds of extracts were identified by GC-MS method. Results: The obtained data showed that the n-Hex extract of E. billardieri on B-16 and MCF7 cell lines and dichromethane extract on MCF7 cell line had the most significant cytotoxic effect compared to DMSO control (p value <0.001). Our finding showed that the mechanism of n-Hex extract with 80% and 100% vlc fractions on B16 induced apoptotic compared to HFF-2 control cells, moreover, n-Hex extract and 80% vlc fraction on MCF7 was apoptotic. The major compounds of n-Hex, DCM and 80% and 100% fractions of n-Hex extract obtained from GC-MS are non-terpenoid. Conclusion: Non-terpenoids compounds of E. billardieri can be the responsible for showing the most cytotoxic effects on MCF7 and B16 cell lines with apoptotic mechanism and n-Hex extract had the most significant inhibitory effect on cancerous cells compared to the HFF-2 control cells by the mechanism of apoptosis.

Diallyl Disulfide Attenuates Methotrexate-Induced Hepatic Oxidative Injury, Inflammation and Apoptosis and Enhances its Anti-tumor Activity

2021 ◽  
Vol 14 ◽  
Author(s):  
Marwa M. Khalaf ◽  
Emad H.M. Hassanein ◽  
Abdel-Gawad S. Shalkami ◽  
Ramadan A.M. Hemeida ◽  
Wafaa R. Mohamed
Keyword(s):  
Cytotoxic Activity ◽  
Caspase 3 ◽  
In Vitro Study ◽  
Diallyl Disulfide ◽  
Sod Activity ◽  
Cytotoxic Effects ◽  
Wide Range ◽  
Anti Tumor Activity ◽  
Mcf 7

Background: Methotrexate (MTX) is used potently for a wide range of diseases. However, hepatic intoxication by MTX hinders its clinical use. Objectives: The present study was conducted to investigate the diallyl disulfide (DADS) ability to ameliorate MTX-induced hepatotoxicity. Methods: Thirty-two rats were randomly divided into four groups: normal control, DADS (50 mg/kg/day, orally), MTX (single i.p. injection of 20 mg/kg) and DADS+MTX. Liver function biomarkers, histopathological examinations, oxidative stress, inflammation, and apoptosis biomarkers were investigated. Besides, an in vitro cytotoxic activity study was conducted to explore the modulatory effects of DADS on MTX cytotoxic activity using Caco-2, MCF-7, and HepG2 cells. Results: DADS significantly reduced the increased serum activities of ALT, AST, ALP, and LDH. These results were confirmed by the alleviation of liver histopathological changes. It restored the decreased GSH content and SOD activity, while significantly decreased MTX-induced elevations in both MDA and NO2- contents. The hepatoprotective effects were mechanistically mediated through the up-regulation of hepatic Nrf-2 and the down-regulation of Keap-1, P38MAPK, and NF-κB expression levels. In addition, an increase in Bcl-2 level with a decrease in the expression of both Bax and caspase-3 was observed. The in vitro study showed that DADS increased MTX anti-tumor efficacy. Conclusions: DADS potently alleviated MTX-induced hepatotoxicity through the modulation of Keap-1/Nrf-2, P38MAPK/NF-κB and apoptosis signaling pathways and effectively enhanced the MTX cytotoxic effects, which could be promising for further clinical trials.

In vitro study of iron coordination properties, anti-inflammatory potential, and cytotoxic effects of N-salicylidene and N-vanillidene anil Schiff bases

2018 ◽  
Vol 72 (9) ◽  
pp. 2171-2180 ◽  
Author(s):  
Zorica D. Petrović ◽  
Jelena Đorović ◽  
Dušica Simijonović ◽  
Snežana Trifunović ◽  
Vladimir P. Petrović
Keyword(s):  
Schiff Bases ◽  
In Vitro Study ◽  
Vitro Study ◽  
Cytotoxic Effects ◽  
Coordination Properties ◽  
Iron Coordination ◽  
Anti Inflammatory

scholarly journals Cytotoxic Activity of Essential Oils of Aerial Parts and Ripe Fruits of Echinophora spinosa (Apiaceae)

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Daniele Fraternale ◽  
Donata Ricci ◽  
Cinzia Calcabrini ◽  
Michele Guescini ◽  
Chiara Martinelli ◽  
...  
Keyword(s):  
Linear Regression ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Central Italy ◽  
U937 Cells ◽  
Cytotoxic Effects ◽  
Regression Curves ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Per Se

The cytotoxic effects of the essential oils obtained from the flowering aerial parts (APO) and ripe fruits (RFO) of Echinophora spinosa L. (Apiaceae) from central Italy toward human U937 promonocytoid cells were studied; the contribution of each of the major constituents to the whole cytotoxic activity of either APO or RFO was also characterized. The major components of APO were β-phellandrene (34.7%), myristicin (16.5%), p-cymene (16.3%), δ3-carene (12.6%), α-pinene (6.7%) and α-phellandrene (6.2%); those of RFO p-cymene (50.2%), myristicin (15.3%), α-pinene (15.1%) and α-phellandrene (8.1%). Both oils tested were toxic to U937 cells, but RFO was much more cytotoxic: indeed, the IC50 values calculated from the linear regression curves of RFO and APO were 14.5 ± 0.85 and 43.4 ± 2.81 μg/mL, respectively. α-Pinene and α-phellandrene were identified as the most toxically relevant constituents: however, they did not completely account for the toxic effects of genuine APO and RFO. Interestingly, we found that p-cymene, although per se devoid of toxicity within the tested range of concentrations, was capable of significantly sensitizing U937 cells to the cytotoxic activity of α-pinene and α-phellandrene, and that specific mixtures of these three terpenes were as toxic as genuine APO and RFO.

Synthesis, crystal structure, and cytotoxic activity of novel cyclic systems in [1,2,4]thiadiazolo[2,3-a]pyridine benzamide derivatives and their copper(ii) complexes

2014 ◽  
Vol 43 (21) ◽  
pp. 7945-7957 ◽  
Author(s):  
Forogh Adhami ◽  
Maliheh Safavi ◽  
Maryam Ehsani ◽  
Sussan K. Ardestani ◽  
Franziska Emmerling ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Planar Structure ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Square Planar ◽  
Benzamide Derivatives

Novel Cu2+complexes with a square planar structure synthesized from benzamide derivatives showed cytotoxic activity against different human cancer cell lines.

scholarly journals Correlation Between Antioxidant and Cytotoxic Activity of Parijoto (Medinilla speciosa Blume) Fractions in 4T1 Cell Line

2021 ◽  
Vol 12 (1) ◽  
pp. 21
Author(s):  
Eva Annisaa' ◽  
Widyandani Sasikirana ◽  
Nuraini Ekawati ◽  
Intan Rahmania Eka Dini
Keyword(s):  
Antioxidant Activity ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Mtt Assay ◽  
Ethyl Acetate Fraction ◽  
Strong Positive Correlation ◽  
Cytotoxic Effects ◽  
Assay Methods ◽  
Botanical Extracts ◽  
Diphenyl Tetrazolium Bromide

Parijoto (Medinilla speciosa Blume) is one of Indonesian plant used for traditional medicine. Previous studies have demonstrated antimicrobial and cytotoxic effects of Parijoto on T47D cells. Therefore, we intended to know the antioxidant and cytotoxic activity of these fractions in 4T1 cell line (a Mus musculus mammary carcinoma). This cancer causes the greatest number of cancer-related deaths This study also investigated the correlation between antioxidant activity and cytotoxicity of Parijoto fractions. Discovering the type of correlation between antioxidant and anticancer activity of botanical extracts could relieve in screening for cytotoxic agent from natural products. The antioxidant and cytotoxic activity investigated using the Diphenylpicrylhydrazyl (DPPH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay methods. The result showed that ethyl acetate fraction is the higher antioxidant activity (IC50:1.77 μg/mL) and the higher cytotoxicity (IC50:133.57 μg/mL). There was a strong positive correlation (correlation coefficient=0.957) between antioxidant and cytotoxic activity in 4T1 cell line, but the correlation was not significant (p=0.188).Keywords: Parijoto (Medinilla speciosa Blume), antioxidant, cytotoxic, 4T1 cell line.

Synthesis of artemisinic acid derived glycoconjugates and their anticancer studies

2020 ◽  
Vol 18 (12) ◽  
pp. 2252-2263
Author(s):  
Tharun K. Kotammagari ◽  
Sayantan Paul ◽  
Ganesh K. Barik ◽  
Manas K. Santra ◽  
Asish K. Bhattacharya
Keyword(s):  
Cell Line ◽  
Mcf7 Cell ◽  
Click Reaction ◽  
Anticancer Activities ◽  
Artemisinic Acid ◽  
Mcf7 Cell Line ◽  
Line P

Twenty-four artemisinic acid glycoconjugate hybrids were synthesized using click reaction and evaluated for their anticancer activities against the MCF7 cell line.

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