scholarly journals Synthesis ,Characterization and invitro evaluation of anticancer activity of new hydroxamicacid basedHDACi containing substituted thaizolesas a cap linking moiety.

2017 ◽  
Vol 13 (10) ◽  
pp. 5954-5961
Author(s):  
Fadil M . Hamed ◽  
Mohammad .H. Mohammad
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Nuclear Extract ◽  
Embryonic Cell ◽  
High Rate ◽  
Hela Nuclear Extract ◽  
H Nmr ◽  
Line Compound ◽  
Derivatives Of

The present study was undertaken to synthesize, characterize  and evaluate the anticancer activity of  new derivatives of hydroxamate –based HDACi  having S-subistituted-5-amino1,3,4thadiazole as a cap linking moiety ,with suitable aliphatic linker.The structures and purity of the targeted compounds were confirmed by TLC , FTIR ,H-NMR and mass spectroscopy and their anticancer activity were evaluated by comparative cytotoxic study , Using HeLa nuclear extract and normal embryonic fibroblasts cell lines.All the synthesized compounds shows good anticancer activity, represented by their high rate of growth inhibition on Hela cell line and low cytotocic effect on normal cell line .Compound (VAb) show the best safety index(SI) that represented by its  selective cytotoxic activity on HeLa cell linewith  low cytotoxic effect on normal embryonic cell line.

scholarly journals Antioxidant and Anticancer Activity of Novel Derivatives of 3-[(4-Methoxyphenyl)amino]propanehydrazide

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 2980 ◽  
Author(s):  
Ingrida Tumosienė ◽  
Kristina Kantminienė ◽  
Arnas Klevinskas ◽  
Vilma Petrikaitė ◽  
Ilona Jonuškienė ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Triple Negative ◽  
Radical Scavenging ◽  
13C Nmr Spectroscopy ◽  
Molecular Structures ◽  
Mass Spectrometry Data ◽  
Derivatives Of ◽  
Dpph Radical Scavenging

Series of novel 3-[(4-methoxyphenyl)amino]propanehydrazide derivatives bearing semicarbazide, thiosemicarbazide, thiadiazole, triazolone, triazolethione, thiophenyltriazole, furan, thiophene, naphthalene, pyrrole, isoindoline-1,3-dione, oxindole, etc. moieties were synthesized and their molecular structures were confirmed by IR, 1H-, 13C-NMR spectroscopy and mass spectrometry data. The antioxidant activity of the synthesized compounds was screened by DPPH radical scavenging method. The antioxidant activity of N-(1,3-dioxoisoindolin-2-yl)-3-((4-methoxyphenyl)amino)propanamide and 3-((4-methoxyphenyl)amino)-N’-(1-(naphthalen-1-yl)-ethylidene)propanehydrazide has been tested to be ca. 1.4 times higher than that of a well-known antioxidant ascorbic acid. Anticancer activity was tested by MTT assay against human glioblastoma U-87 and triple-negative breast cancer MDA-MB-231 cell lines. In general, the tested compounds were more cytotoxic against U-87 than MDA-MB-231 cell line. 1-(4-Fluorophenyl)-2-((5-(2-((4-methoxyphenyl)amino)ethyl)-4-phenyl-4H-1,2,4-triazol-3-yl)thio)ethanone has been identified as the most active compound against the glioblastoma U-87 cell line.

scholarly journals In vitro Anticancer Activity Effect of Extracellular Metabolites of Some Bacterial Species on HeLa Cell Line.

2020 ◽  
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Hela Cells ◽  
Bacterial Species ◽  
Hela Cell Line ◽  
Inhibitory Effects ◽  
Anticancer Effect ◽  
E Coli ◽  
Extracellular Metabolites

Background: Cancer is still one of the most serious problems that affect human health. Despite the intense efforts to develop treatments, effective agents are still not available. In some cases, conventional therapy could be harmful or fail because of emerging drug resistance. Therefore, the development of novel therapies against cancer is of utmost importance. Assessment of anticancer effects of bacterial metabolites on cancer cells may help in the process of finding new cheap, reliable, contentious and safe cancer therapy. Objective: To determine the anticancer effect of the extracellular metabolites of eight bacterial species on HeLa cell line. Methodology: Extracellular metabolites were prepared by isolating and culturing eight bacterial species (Escherichia coli, Staphylococcus aureus, Micrococcus, Pseudomonas aeruginosa, Lactic acid bacteria, Klebsiella, Proteus and E. coli with its phage) in liquid media. Tubes were incubated overnight and centrifuged. Supernatant was filtered and concentrated using Infra-Red concentrator. Different concentrations were prepared and their anticancer effect were evaluated using MTT cell proliferation assay. Results: Results showed variation among the eight bacteria concerning proliferation inhibition against HeLa cells in a time and concentration dependent manner. Pseudomonas and E. coli with its phage revealed considerable anticancer activity with 63% and 86% inhibitory effects (both at 1000 µg\ml) and IC50 of 301 and 1395 µg/dl at 24h respectively. While Proteus and Micrococcus showed low inhibitory effects and S. aureus enhanced the proliferation of HeLa cells at low concentrations. Conclusion: Among the tested bacteria, Pseudomonas and E. coli and its phage gave the best anticancer inhibitory effects against HeLa cells. Further studies using purified components of effective bacteria are recommended.

scholarly journals Total synthesis and anticancer activity of the natural oleanolic acid bidesmoside saponin, albidoside A, isolated from the roots of Acacia albida

2019 ◽  
Vol 44 (1-2) ◽  
pp. 42-49
Author(s):  
Tiantian Guo ◽  
Yiming Song ◽  
Yinghui Lu ◽  
Guolin Li ◽  
Tian Liu ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Oleanolic Acid ◽  
Triterpenoid Saponin ◽  
Hela Cell Line ◽  
Hela Cell Lines ◽  
Acacia Albida ◽  
Mcf 7

The first synthesis of a natural triterpenoid saponin bearing N-acetylglucosamine, albidoside A, which is isolated from the roots of Acacia albida, is concisely achieved in a convergent strategy. Preliminary pharmacological research shows anticancer activity against HL-60, MCF-7, MDA-MB-231, Hep-2, and Hela cell lines. In particular, it exhibited good selectivity, which is five times more cytotoxic toward Hep-2 cells (IC50 = 8.91 μM) than the Hela cell line.

Anticancer Activity of Aminoacid Linked Novel 4-Methylumbelliferone Derivatives

2019 ◽  
Vol 15 (1) ◽  
pp. 51-62 ◽  
Author(s):  
Manish Sinha ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Shruti Kuletha ◽  
Karanveer Singh ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Inhibitory Effect ◽  
Central Nucleus ◽  
Core Nucleus ◽  
Line Compound ◽  
Assay Protocol

Background: Cancer is a disease of high mortality. The therapeutic agents currently available are insufficient to cure it and are associated with serious side effects. 4-methylumbelliferone is a natural product containing benzo-α-pyrones as a central nucleus. Benzo-α-pyrone is a privileged moiety having multifarious biological activities including anticancer activity. A series of compounds were synthesized taking 4-methylumbelliferone as a core nucleus and screened for their anticancer activity against HeLa cancer cell line. Methods: The 4-methylumbelliferone was linked with aminoacids using chloroacetyl chloride or ethyl chloroacetate as linker. The N-methylmorpholine and isobutylchloroformate protocol was used for amidic coupling. The final compounds were tested against the HeLa cancer cell lines using SRB assay protocol. Results: Three compounds have shown significant anticancer activity viz 9a, 12f and 15l having GI50 (µg/ml) value of, 56.1, 30.9 and 50.9, respectively. Other compound 9f and 13 showed weak anticancer activity having GI50 (µg/ml) value of 97.2 and 71.1, respectively. Conclusion: It has been found that the synthesized derivatives have inhibitory effect on the growth of cancer cell line. Compound 12f has been found as the most active compound of the synthesized series.

Heteroleptic Pd(II) dithiocarbamates: synthesis, characterization, packing and in vitro anticancer activity against HeLa cell line

2015 ◽  
Vol 68 (14) ◽  
pp. 2539-2551 ◽  
Author(s):  
Shahan zeb Khan ◽  
Muhammad Kashif Amir ◽  
Muhammad Moazzam Naseer ◽  
Rashda Abbasi ◽  
Kehkashan Mazhar ◽  
...  
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Hela Cell Line

scholarly journals Anticancer Evaluation of Plants from Indonesian Tropical Rain Forests

2011 ◽  
Vol 2 (3) ◽  
pp. 310
Author(s):  
Jamilah Abbas
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Stem Bark ◽  
Tropical Rainforests ◽  
Hela Cell Line ◽  
Tropical Rain Forests ◽  
Rain Forests ◽  
Anticancer Activities ◽  
Ic50 Value

The anticancer activities of medicinal plants from Indonesia’s tropical rainforests were investigated against Hela cell line. Maytenfoliol from leaves of Calophyllumtetrapterum 3-epibetulinic acid from stem bark of C. tomentosum Wight and D.A-friedo-oleanan-3-on from stem bark of C. moonii showed anticancer activity. The compound 3-epibetulinic acid showed the more potent anticancer activity than maytenfoliol and D.A-friedo-oleanan-3- with thean IC50 value were 3.17 μg/mL, 4.89 μg/mL and 5.63 μg/mL, respectively.Keywords: Anticancer evaluation, Hela cell line, Calophyllumtetrapterum. C. tomentosum Wight and C. moonii

Synthesis, Characterization, Biological Evaluation and Molecular Docking Studies of New Oxoacrylate and Acetamide on heLa Cancer Cell Lines

2020 ◽  
Vol 16 ◽  
Author(s):  
Nevin Çankaya ◽  
Mehmetcan İzdal ◽  
Serap Yalçin Azarkan
Keyword(s):  
Molecular Docking ◽  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Critical Role ◽  
Biological Evaluation ◽  
New Drugs ◽  
Hela Cell Line ◽  
Molecular Docking Study

Background: In recent years, discovery and development of new drugs play a critical role in cancer therapy. Objective: In this study, the effect of MPAEA and p-acetamide on cellular toxicity and on silico in HeLa cancer cells have been investigated. Methods: In this study, 2-choloro-N-(4-methoxyphenyl)acetamide (p-acetamide) and 2-(4-methoxyphenylamino)-2- oxoethyl acrylate (MPAEA) have been synthesized and characterized by FTIR, 1H, and 13C-NMR. Cytotoxicity of pacetamide and MPAEA have been investigated by XTT cell proliferation assay on the HeLa cell line. IC50 values of pacetamide and MPAEA have been identified on the HeLa cell line. Further, molecular docking study was carried out by Autodock Vina using BCL-2 (PDB ID: 4MAN), BCL-W (PDB ID: 2Y6W), MCl-1 (PDB ID: 5FDO) AKT (PDB ID: 4GV1) and BRAF (PDB ID: 5VAM) as a possible apoptotic target for anticancer activity. Results: According to the obtained results, MPAEA and p-acetamide were successfully synthesized and characterized. The interactions between ligands and anti-apoptotic proteins were evaluated by molecular docking and their free energy of binding were calculated and used as descriptor. Conclusion: In vitro and in silico the results demonstrated that MPAEA had potent anticancer activity on HeLa cell line.

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