Syntheses and Cytotoxicity Screening of some Novel 1,2,4-Triazine Derivatives against Liver Carcinoma Cell Lines

2020 ◽  
Vol 17 ◽  
Author(s):  
W. Abd El-Fattah
Keyword(s):  
Acetic Anhydride ◽  
Cell Lines ◽  
Carcinoma Cell ◽  
Aromatic Aldehydes ◽  
Liver Carcinoma ◽  
Anticancer Activities ◽  
Carcinoma Cell Lines ◽  
Elemental Analyses ◽  
Triazine Derivatives ◽  
C Nmr

: In this work, 1,2,4-triazine derivatives were synthesized and evaluated for anticancer activities. Series of 1,2,4-triazine derivatives (4a, b) were prepared via the reaction of N-benzoyl glycine (1) with aromatic aldehydes in presence of fused sodium acetate and acetic anhydride to give 1,3-oxazolinone derivatives (2a, b), followed by condensation with 1-(ethoxycarbonyl) hydrazine (3) in glacial acetic acid. Compounds (4a, b) then reacted with acetic anhydride, ethyl chloroacetate and 2,4-dinitrophenyl hydrazine yielded the corresponding to N-acetyl derivatives (5a, b), N-(ethoxycarbonyl) methyl derivative (6) and 1,2-disubstituted hydrazine (7), respectively. The structures of the 1,2,4-triazine derivatives were confirmed by IR, 1H, 13C NMR, MS and elemental analyses. Anticancer activity of some 1,2,4-triazine derivatives (4-7) have been investigated. The results revealed that compounds 4a (IC50= 2.7μM), 5a (IC50= 1.5μM), and 5b (IC50= 3.9μM) show promising inhibitory growth efficacy compared to a standard antitumor drug (IC50= 4.6μM). These three compounds can be considered as potential agents against human hepatocellular carcinoma cell lines (HepG-2).

The Synthesis and Anticancer Activities of Peptide 5-fluorouracil Derivatives

2009 ◽  
Vol 2009 (4) ◽  
pp. 261-264 ◽  
Author(s):  
Xiaowei Yan ◽  
Maolin Hu ◽  
Qian Miao ◽  
Shun Wang ◽  
Kejian Zhao
Keyword(s):  
Cell Lines ◽  
Mass Spectra ◽  
Anticancer Activities ◽  
H Nmr ◽  
Elemental Analyses ◽  
C Nmr

A new series of peptide 5-fluorouracil derivatives was designed and synthesised in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses.

scholarly journals ID: 1012 Cytotoxicity of Corchorus olitorius Linn. aqueous leaf extract against human carcinoma cells

2017 ◽  
Vol 4 (S) ◽  
pp. 86
Author(s):  
John Paul Tosoc
Keyword(s):  
Cell Viability ◽  
Cell Line ◽  
Cell Lines ◽  
Aqueous Extract ◽  
Carcinoma Cell ◽  
Carcinoma Cell Line ◽  
Liver Carcinoma ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Viability Percentage

C. olitorius are used as herbal medicine and eaten as vegetable by local people in Philippines.  The T’boli tribe commonly uses this plant to treat common illnesses such as pimples, wounds, boils, and inflammations. According to studies, the leaves of C. olitorius has properties to treat demulcent, diuretic, febrifuge, chronic cystitis, dysuria and even tumor. The aim of this study is to evaluate the cytotoxicity properties of the crude aqueous extract of C. olitorius leaf against colon (HCT116), breast (MCF-7), and liver (HepG2) carcinoma cell-lines using the MTT cell proliferation assay. The results showed that the aqueous extract has potential cytotoxicity activity against the three-carcinoma cell-lines. The aqueous extract was most bioactive in the colon carcinoma cell-line (HCT116) with cell viability percentage of 23.53 and 32.48 in 100 and 10 µg/mL, respectively. It was then followed by the breast carcinoma cell-line (MCF7) with cell viability percentage of 16.23 and 30.25 in 100 and 10 µg/mL, respectively. The extract was least but still bioactive in the liver carcinoma cell-line (HepG2) with cell viability percentage of 91.20 and 132.76 in 100 and 10 µg/mL, respectively. This study illustrates the importance of toxicological screening to confirm the safety and efficacy of the medicinal plant commonly used in the traditional medicine system in the treatment and management of illnesses by the T’boli tribe in South Cotabato

scholarly journals Synthesis of Novel VO(II)-Perimidine Complexes: Spectral, Computational, and Antitumor Studies

2018 ◽  
Vol 2018 ◽  
pp. 1-22 ◽  
Author(s):  
Gamil A. Al-Hazmi ◽  
Khlood S. Abou-Melha ◽  
Nashwa M. El-Metwaly ◽  
Kamel A. Saleh
Keyword(s):  
Cell Lines ◽  
Metal Ion ◽  
Carcinoma Cell ◽  
Xrd Analysis ◽  
Sem Analysis ◽  
Liver Carcinoma ◽  
Sem Images ◽  
Carcinoma Cell Lines ◽  
Coordination Spheres ◽  
Ct Dna

A series of perimidine derivatives (L1–5) were prepared and characterized by IR, 1H·NMR, mass spectroscopy, UV-Vis, XRD, thermal, and SEM analysis. Five VO(II) complexes were synthesized and investigated by most previous tools besides the theoretical usage. A neutral tetradentate mode of bonding is the general approach for all binding ligands towards bi-vanadyl atoms. A square-pyramidal is the configuration proposed for all complexes. XRD analysis introduces the nanocrystalline nature of the ligand while the amorphous appearance of its metal ion complexes. The rocky shape is the observable surface morphology from SEM images. Thermal analysis verifies the presence of water of crystallization with all coordination spheres. The optimization process was accomplished using the Gaussian 09 software by different methods. The most stable configurations were extracted and displayed. Essential parameters were computed based on frontier energy gaps with all compounds. QSAR parameters were also obtained to give another side of view about the biological approach with the priority of the L3 ligand. Applying AutoDockTools 4.2 program over all perimidine derivatives introduces efficiency against 4c3p protein of breast cancer. Antitumor activity was screened for all compounds by a comparative view over breast, colon, and liver carcinoma cell lines. IC50 values represent promising efficiency of the L4-VO(II) complex against breast, colon, and liver carcinoma cell lines. The binding efficiency of ligands towards CT-DNA was tested. Binding constant (Kb) values are in agreement with the electron-drawing character of the p-substituent which offers high Kb values. Also, variable Hammett’s relations were drawn.

scholarly journals Cytotoxic Xanthones from Hypericum stellatum, an Ethnomedicine in Southwest China

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3568 ◽  
Author(s):  
Ji ◽  
Zhang ◽  
Zhang ◽  
Li ◽  
Negrin ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Liver ◽  
Carcinoma Cell ◽  
Positive Control ◽  
Guizhou Province ◽  
Liver Carcinoma ◽  
Aerial Parts ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Relationship Of

Hypericum stellatum, a species endemic to China, is used to treat hepatitis by several ethnic groups in Guizhou Province. This research was inspired by the traditional medicinal usage of H. stellatum, and aims to explore the phytochemistry and bioactivity of H. stellatum to explain why local people in Guizhou widely apply H. stellatum for liver protection. In this study, two new prenylated xanthones, hypxanthones A (8) and B (9), together with seven known compounds, were isolated from the aerial parts of the plant. Spectroscopic data as well as experimental and calculated ECD spectra were used to establish the structures of these compounds. Six xanthones isolated in this study, together with four xanthones previously isolated from H. stellatum, were evaluated for their growth-inhibitory activities against five human liver carcinoma cell lines to analyze the bioactivity and structure-activity relationship of xanthones from H. stellatum. Isojacareubin (6) showed significant cytotoxicity against five human liver carcinoma cell lines, with an IC50 value ranging from 1.41 to 11.83 μM, which was stronger than the positive control cisplatin (IC50 = 4.47–20.62 μM). Hypxanthone B (9) showed moderate cytotoxicity to three of the five cell lines. Finally, structure-activity analysis revealed that the prenyl and pyrano substituent groups of these xanthones contributed to their cytotoxicity.

Disruption of microfilaments by cytochalasin B decreases accumulation of cisplatin in human epidermal carcinoma and liver carcinoma cell lines

2008 ◽  
Vol 62 (6) ◽  
pp. 977-984 ◽  
Author(s):  
Xing-Jie Liang ◽  
Jun-Jie Yin ◽  
Barbara Taylor ◽  
Stephen M. Winkovitch ◽  
Susan H. Garfield ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cytochalasin B ◽  
Carcinoma Cell ◽  
Liver Carcinoma ◽  
Carcinoma Cell Lines ◽  
Epidermal Carcinoma

Ten new primary pancreatic carcinoma cell lines

2011 ◽  
Vol 49 (08) ◽  
Author(s):  
F Rückert ◽  
D Aust ◽  
S Hering ◽  
K Werner ◽  
HD Saeger ◽  
...  
Keyword(s):  
Pancreatic Carcinoma ◽  
Cell Lines ◽  
Carcinoma Cell ◽  
Carcinoma Cell Lines
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