Synthesis, characterization, and anticancer evaluation of some new N1-(anthraquinon-2-yl) amidrazone derivatives

2018 ◽  
Vol 96 (12) ◽  
pp. 1123-1128 ◽  
Author(s):  
Kamal Sweidan ◽  
Hiba Zalloum ◽  
Dima A. Sabbah ◽  
Ghada Idris ◽  
Khadija Abudosh ◽  
...  
Keyword(s):  
Cell Lines ◽  
Dermal Fibroblasts ◽  
Myelogenous Leukemia ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
A Cell ◽  
New Compounds ◽  
Mcf 7

A new series of novel N1-anthraquinon-2-yl amidrazones incorporating N-piperazines and related congeners were synthesized via reaction of the hydrazonoyl chloride derived from 2-qaminoanthraquinone with the appropriate piperazine (secondary amine). Structures of the new compounds were confirmed by a panel of spectroscopic methods including IR, NMR, and MS and by elemental analysis. The antitumor activity of the newly prepared compounds was evaluated in vitro against MCF-7 breast cancer, K562 chronic myelogenous leukemia, and dermal fibroblasts cell lines by means of a cell viability assay using the tetrazolium dye 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Results revealed that compounds 13a and 13d exhibit the highest inhibitory activity against K562 and MCF-7 cell lines. These two compounds could be considered as promising as potential anticancer drugs.

scholarly journals Synthesis, Characterization, and Anticancer Activity of New Benzofuran Substituted Chalcones

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Demet Coşkun ◽  
Suat Tekin ◽  
Süleyman Sandal ◽  
Mehmet Fatih Coşkun
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Cell Viability Assay ◽  
Anticancer Properties ◽  
Viability Assay ◽  
Diphenyltetrazolium Bromide ◽  
Antitumor Properties ◽  
Mcf 7

Benzofuran derivatives are of great interest in medicinal chemistry and have drawn considerable attention due to their diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures of numerous natural products belonging to the flavonoid class, feature strong anticancer properties. A novel series of chalcones, 3-aryl-1-(5-bromo-1-benzofuran-2-yl)-2-propanones propenones (3a–f), were designed, synthesized, and characterized.In vitroantitumor activities of the newly synthesized (3a–f) and previously synthesized (3g–j) chalcone compounds were determined by using human breast (MCF-7) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested chalcone compounds was performed and thelog⁡IC50values of the compounds were calculated after 24-hour treatment. Our results indicate that the tested chalcone compounds show antitumor activity against MCF-7 and PC-3 cell lines (p<0.05).

Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones

2014 ◽  
Vol 69 (7) ◽  
pp. 811-816 ◽  
Author(s):  
Mohammed M. Abadleh ◽  
Mustafa M. El-Abadelah ◽  
Salim S. Sabri ◽  
Hanan H. Mohammed ◽  
Malek A. Zihlif ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antitumor Activity ◽  
Cell Viability ◽  
Cell Lines ◽  
K562 Cell ◽  
Cyclic Amine ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
A Cell ◽  
Mcf 7

6aA set of new N2-(thien-3-yl)amidrazones (-h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4(derived from 3-aminothiophene- 2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9:91 μM, respectively.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

scholarly journals A2AR Antagonists Upregulate Expression of GS and GLAST in Rat Hypoxia Model

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Jun Yu ◽  
Yan Yan ◽  
Yiye Chen ◽  
Yan Zheng ◽  
Xiaoyan Yu ◽  
...  
Keyword(s):  
Müller Cells ◽  
Muller Cells ◽  
Cell Viability Assay ◽  
Hypoxic Conditions ◽  
Viability Assay ◽  
Drug Concentrations ◽  
A Cell ◽  
Short Time

Background. The aim of this study was to research the effects of glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) in rat Müller cells and the effects of an adenosine A2AR antagonist (SCH 442416) on GS and GLAST in hypoxia both in vivo and in vitro. Methods. This study used RT-PCR and Western blotting to quantify the expressions of GS and GLAST under different hypoxic conditions as well as the expressions of GS and GLAST at different drug concentrations. A cell viability assay was used to assess drug toxicity. Results. mRNA and protein expression of GS and GLAST in hypoxia Group 24 h was significantly increased. mRNA and protein expressions of GS and GLAST both increased in Group 1 μM SCH 442416 compared with other groups. One micromolar SCH 442416 could upregulate GS and GLAST’s activity in hypoxia both in vivo and in vitro. Conclusions. Hypoxia activates GS and GLAST in rat retinal Müller cells in a short time in vitro. (2) A2AR antagonists upregulate the activity of GS and GLAST in hypoxia both in vivo and in vitro.

scholarly journals In vitro evaluation of the activity of terpenes and cannabidiol against Human Coronavirus E229

2021 ◽  
Author(s):  
Lior Chatow ◽  
Adi Nudel ◽  
Iris Nesher ◽  
David Hayo Hemo ◽  
Perri Rozenberg ◽  
...  
Keyword(s):  
Antiviral Effect ◽  
Host Cells ◽  
Lung Fibroblasts ◽  
Human Coronavirus ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
A Cell ◽  
Quantitative Results ◽  
Better Than

AbstractThe activity of a new, terpene-based formulation, code-named NT-VRL-1, against Human Coronavirus (HCoV) strain 229E was evaluated in human lung fibroblasts (MRC-5 cells), with and without the addition of cannabidiol (CBD). The tested formulation exhibited an antiviral effect when it was pre-incubated with the host cells prior to virus infection. The combination of NT-VRL-1 with CBD potentiated the antiviral effect better than the positive controls pyrazofurin and glycyrrhizin. There was a strong correlation between the quantitative results from a cell-viability assay and the cytopathic effect seen under the microscope after 72 h. To the best of our knowledge, this is the first report of activity of a combination of terpenes and CBD against a coronavirus.

Evaluation of the Influence of Ferrite Magnetic Nanoparticle for Cancer Cell

2021 ◽  
Vol 323 ◽  
pp. 146-151
Author(s):  
Khishigdemberel Ikhbayar ◽  
Nomin Myagmar ◽  
Gantulga Davaakhuu ◽  
Uyanga Enkhnaran ◽  
Enkhmend Bekhbaatar ◽  
...  
Keyword(s):  
Cell Viability ◽  
Colony Formation ◽  
Magnetic Nanoparticle ◽  
In Vitro Cytotoxicity ◽  
Colony Formation Assay ◽  
Cell Viability Assay ◽  
Cytotoxic Effects ◽  
Viability Assay ◽  
A Cell

Magnetic nanoparticles for thermotherapy must be biocompatible and possess high thermal efficiency as heating elements. The biocompatibility of Mg 0.8 Ni 0.2 Fe 2 O 4 nanoparticles was studied using a cytotoxicity colony formation assay and a cell viability assay. HeLa cells exhibited cytotoxic effects when exposed to three different concentrations of 150 μg /ml, 100 μg /ml, and 50 μg /ml nanoparticles. Therefor e, c oncentrations of 50 μg /ml showed the lowest cytotoxic activity and the lowest toxicity to living cells. In vitro cytotoxicity of samples was then investigated by two methods, colony formation assay and cell viability assay. The Hela inhibited cell growth as 16.8% during heating by magnetic field generators.

scholarly journals Anti-HIV Activity of MDL 74968, a Novel Acyclonucleotide Derivative of Guanine: Drug Resistance and Drug Combination Effects in Vitro

1996 ◽  
Vol 7 (5) ◽  
pp. 253-260 ◽  
Author(s):  
D.L. Taylor ◽  
S.P. Ahmed ◽  
T.M. Brennan ◽  
J.-F. Navé ◽  
P. Casara ◽  
...  
Keyword(s):  
Nucleoside Analogues ◽  
Drug Resistant ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Immunodeficiency Virus ◽  
A Cell ◽  
Experimental Protocols ◽  
Hiv 1

MDL 74968 (9-[2-methylidene-3-(phosphonomethoxy)-propyl]guanine), a novel acyclonucleotide derivative of guanine, inhibited human immunodeficiency virus type 1 (HIV-1) replication in vitro with activity comparable to that of adefovir (PMEA; 9-(2-phosphonomethoxyethyl)adenine). MDL 74968 was investigated in combination with two licensed nucleoside analogues, zidovudine and didanosine, using a cell viability assay, and drug interactions were evaluated by the isobologram technique, by calculating combination indices and by the MacSynergy™ program. Inhibition of HIV-1 replication was only additive in both cases. MDL 74968 had equivalent antiviral activity against strains of HIV-1 HXB2 engineered to have mutations which conferred resistance to the nucleoside analogues lamivudine, didanosine and zidovudine and the non-nucleoside inhibitor of reverse transcriptase (RT) nevirapine, as against the wild type strain. Continued passage of HIV-1 RF in C8166 cells in the presence of MDL 74968 for 5 months (30 passages) failed to select drug resistant mutants. Continued passage of virus in the presence of the same concentration of adefovir for the same length of time selected a virus in a single culture, which was 3-fold resistant to adefovir and cross-resistant to MDL 74968. Genotypic characterization of this virus revealed a lysine to arginine exchange (AAA to AGA) at position 65 in the RT gene. This virus was not cross-resistant to either zidovudine or nevirapine but showed reduced sensitivity to zalcitabine, didanosine and lamivudine. Continued passage of HIV-1 RF in the presence of nevirapine or zidovudine, using similar experimental protocols selected drug resistant viruses after eight and 17 passages, respectively, but these viruses remained sensitive to adefovir and MDL 74968.

scholarly journals In Vitro Evaluation of the Activity of Terpenes and Cannabidiol against Human Coronavirus E229

Life ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 290
Author(s):  
Lior Chatow ◽  
Adi Nudel ◽  
Iris Nesher ◽  
David Hayo Hemo ◽  
Perri Rozenberg ◽  
...  
Keyword(s):  
Antiviral Effect ◽  
Host Cells ◽  
Lung Fibroblasts ◽  
Human Coronavirus ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
A Cell ◽  
Quantitative Results ◽  
Better Than

The activity of a new, terpene-based formulation, code-named NT-VRL-1, against Human Coronavirus (HCoV) strain 229E was evaluated in human lung fibroblasts (MRC-5 cells), with and without the addition of cannabidiol (CBD). The main constituents in the terpene formulation used for the experiment were beta caryophyllene, eucalyptol, and citral. The tested formulation exhibited an antiviral effect when it was pre-incubated with the host cells prior to virus infection. The combination of NT-VRL-1 with CBD potentiated the antiviral effect better than the positive controls pyrazofurin and glycyrrhizin. There was a strong correlation between the quantitative results from a cell-viability assay and the cytopathic effect seen under the microscope after 72 h. To the best of our knowledge, this is the first report of activity of a combination of terpenes and CBD against a coronavirus.

scholarly journals Synthesis, Structural Characterization and Anticancer Activity of New 5-Trifluoromethyl-2-thioxo-thiazolo[4,5-d]pyrimidine Derivatives

2022 ◽  
Vol 15 (1) ◽  
pp. 92
Author(s):  
Lilianna Becan ◽  
Anna Pyra ◽  
Nina Rembiałkowska ◽  
Iwona Bryndal
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Screening Program ◽  
Human Cancer ◽  
3D Structure ◽  
X Ray Diffraction ◽  
Pyrimidine Derivatives ◽  
New Compounds ◽  
Mcf 7

Thiazolo[4,5-d]pyrimidine derivatives are considered potential therapeutic agents, particularly in the development of anticancer drugs. In this study, new 7-oxo-(2a-e), 7-chloro-(3a-e) and also three 7-amino-(4a-c) 5-trifluoromethyl-2-thioxo-thiazolo[4,5-d]pyrimidine derivatives have been synthesized and evaluated for their potential anticancer activity. These derivatives were characterized by spectroscopic methods and elemental analysis, and the single-crystal X-ray diffraction was further performed to confirm a 3D structure for compounds 2e and 4b. The antiproliferative activity evaluation of twelve new compounds was carried out on a variety of cell lines including four human cancer (A375, C32, DU145, MCF-7/WT) and two normal cell lines (CHO-K1 and HaCaT). Four of them (2b, 3b, 4b and 4c) were selected by the National Cancer Institute and evaluated for their in vitro anticancer activity using the NCI-60 screening program. 7-Chloro-3-phenyl-5-(trifluoromethyl)[1,3]thiazolo[4,5-d]pyrimidine-2(3H)-thione (3b) proved to be the most active among the newly synthesized compounds.

scholarly journals Effect of Metalloprotease Arazyme on the Expression of MMP2 and MMP9 Genes in Metastasis of Colon and Ovarian Cancer Cell Lines

Thrita ◽  
2020 ◽  
Vol 8 (2) ◽  
Author(s):  
Ghazaleh Amjadi ◽  
Kazem Parivar ◽  
Seyed Fazlollah Mousavi ◽  
Abbas Ali Imani Fooladi
Keyword(s):  
Ovarian Cancer ◽  
Cell Lines ◽  
The United States ◽  
Culture Cell ◽  
Bacterial Strains ◽  
Antitumor Effects ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Common Cancer

Background: After cardiovascular diseases, cancer is the main cause of death in the United States, and its prevalence is continually increasing. Ovarian cancer is a fetal and common cancer among women and is the eighth common cancer in Iran. Colorectal cancer is known as the second and fourth common cancer in Iranian women and men, respectively. Arazyme is a metalloprotease with strong antitumor effects on tumor cells. Objectives: This study aimed at studying the effect of metalloprotease arazyme in vitro on the expression of MMP2 and MMP9 genes, causing metastasis in ovarian and colon cancer. Methods: Bacterial strains and cell lines, the construction of an expression vector, and preparation of recombinant protein were done. Then, they were evaluated by Western blot, cell culture, cell viability assay, and reverse transcriptase-polymerase chain reaction. Results: The effects of arazyme on ovarian and colon cell lines were assessed by the MTT assay showing that the viability of cancer cells treated with arazyme decreased significantly in comparison with control cells. Also, RT-PCR showed that the expression of MMP2 and MMP9 genes decreased after treatment with arazyme, which was significant when compared to the results of pre-treatment. Conclusions: In this study, the results showed that the use of arazyme protein as a bacterial anti-protease can play a significant role in reducing the expression of metastatic genes. According to numerous studies on the role of bacterial proteases in the process of metastasis in recent years, this method can be considered as a therapeutic approach in reducing the metastatic process.

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