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, 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 Preparation, Characterization, and Anticancer Effects of Capsaicin-Loaded Nanoliposomes

Nutrients ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 3995
Author(s):  
Ali Al-Samydai ◽  
Walhan Alshaer ◽  
Emad A. S. Al-Dujaili ◽  
Hanan Azzam ◽  
Talal Aburjai
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Therapeutic Potential ◽  
Drug Loading ◽  
Cell Viability Assay ◽  
Viability Assay ◽  
Anticancer Effects ◽  
Pharmacokinetic Properties ◽  
Quantitative Analyses

Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

scholarly journals A Nitrocarbazole as a New Microtubule-Targeting Agent in Breast Cancer Treatment

2021 ◽  
Vol 11 (19) ◽  
pp. 9139
Author(s):  
Maria Stefania Sinicropi ◽  
Cinzia Tavani ◽  
Camillo Rosano ◽  
Jessica Ceramella ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Breast Cancer Cell Lines ◽  
Cellular Functions ◽  
Anticancer Properties ◽  
Cycle Arrest ◽  
In Silico Studies ◽  
Ic50 Values ◽  
Mcf 7

Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, such as microtubule components. The latter are involved in vital cellular functions, and the perturbation of their dynamics leads to cell cycle arrest and subsequent apoptosis. In this context, we report the anticancer activity of a series of carbazole analogues 1–8. Among them, 2-nitrocarbazole 1 exhibited the best cytotoxic profile, showing good anticancer activity against two breast cancer cell lines, namely MCF-7 and MDA-MB-231, with IC50 values of 7 ± 1.0 and 11.6 ± 0.8 μM, respectively. Furthermore, compound 1 did not interfere with the growth of the normal cell line MCF-10A, contrarily to Ellipticine, a well-known carbazole derivative used as a reference molecule. Finally, in vitro immunofluorescence analysis and in silico studies allowed us to demonstrate the ability of compound 1 to interfere with tubulin organization, similarly to vinblastine: a feature that results in triggering MCF-7 cell death by apoptosis, as demonstrated using a TUNEL assay.

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.

Influence of amide versus ester linkages on the anticancer properties of the new flavone–biotin conjugates

2019 ◽  
Vol 74 (7-8) ◽  
pp. 193-200
Author(s):  
Monika Stompor ◽  
Marta Świtalska ◽  
Agata Bajek ◽  
Joanna Wietrzyk
Keyword(s):  
Cell Lines ◽  
Amide Bond ◽  
Step Method ◽  
Fluorescent Reporter ◽  
Bifunctional Molecules ◽  
Anticancer Properties ◽  
One Step ◽  
3T3 Cell Lines ◽  
Mcf 7

Abstract Novel biotinylated C-6 substituted flavones were synthesised by a one-step method that connects biotin to 6-hydroxyflavone and 6-aminoflavone by esterification and amidation of hydroxyl and amino groups, respectively. The obtained compounds, 6-O-biotinylflavone and 6-biotinylamidoflavone, are the bifunctional molecules composed of a flavone moiety as a fluorescent reporter and biotin as a cancer-targeting unit. Antiproliferative activity was evaluated using SRB assays in MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1, and Balb/3T3 cell lines. In vitro evaluation revealed that compounds with biotin moiety displayed better cell selectivity between the cancer and normal cells than the parental substrates. These results indicate that anticancer effect is not related to the position of biotin moiety, but it is related to the presence of ester or amide bond. 6-O-Biotinylflavone was more active than 6-hydroxyflavone against human breast (MDA-MB-231) and liver (HepG2) cancer cells with IC50 (concentration of tested agent that inhibits proliferation of the cell population by 50%) values equal to 78.5 ± 18.8 μM and 133.2 ± 14.2 μM, respectively. Non biotinylated 6-aminoflavone was more active than 6-biotinylamidoflavone against all tested cell lines, with IC50 values between 34.3 ± 9.1 μM (4T1) and 173.86 ± 24.3 μM (MCF-7).

scholarly journals Synthesis, Characterization, and In Vitro Cancer Cell Growth Inhibition Evaluation of Novel Phosphatidylcholines with Anisic and Veratric Acids

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2022 ◽  
Author(s):  
Marta Czarnecka ◽  
Marta Świtalska ◽  
Joanna Wietrzyk ◽  
Gabriela Maciejewska ◽  
Anna Gliszczyńska
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Human Organism ◽  
Cancer Cell Growth ◽  
Anticancer Properties ◽  
Health Promoting ◽  
Phenolcarboxylic Acids ◽  
Mcf 7

Phenolic acids and its methoxy derivatives are known to induce caspase-mediated apoptosis activity and exhibit cytotoxic effect towards various cancer cell lines. However, their low stability and poor bioavailability in the human organism extensively restrict the utility of this group of compounds as anticancer and health-promoting agents. In this report, a series of eight novel phosphatidylcholines (3a-b, 5a-b, 7a-b, 8a-b) containing anisic or veratric acids (1a-b) at sn-1 and/or sn-2 positions were synthesized. The phenoylated phospholipids were obtained in good yields 28–66%. The structures of novel compounds were determined by their spectroscopic data. All synthesized compounds were evaluated for their antiproliferative activity towards six cancer cell lines and normal cell line Balb/3T3. Lipophilization of phenolcarboxylic acids significantly increased their anticancer properties. The asymmetrically substituted phenoylated phosphatidylcholines exhibited higher antiproliferative effect than free acids. Lysophosphatidylcholine (7b) effectively inhibited the proliferation of human leukaemia (MV4-11), breast (MCF-7), and colon (LoVo) cancer cell lines at concentrations of 9.5–20.7 µm and was from 19 to 38-fold more active than corresponding free veratric acid. The conjugation of anisic/veratric acids with the phosphatidylcholine have proved the anticancer potential of these phenolcarboxylic acids and showed that this type of lipophilization is an effective method for the production of active biomolecules.

scholarly journals Porous Cu-MOF Nanostructures with Anticancer Properties Prepared by a Controllable Ultrasound-Assisted Reverse Micelle Method

2021 ◽  
Author(s):  
Malihe Zeraati ◽  
Mohammadreza Moghaddam-Manesh ◽  
Sara Hosseinzadegan ◽  
Parya Kazemzadeh ◽  
Narendra Pal Singh Chauhan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Reverse Micelle ◽  
Breast Cancer Cells ◽  
Nitrogen Adsorption ◽  
Cell Viability Assay ◽  
Anticancer Properties ◽  
Viability Assay ◽  
Ultrasonic Assisted ◽  
Mcf 7

Abstract The ultrasonic assisted reverse micelle method was used to create Cu-MOF from Cu(NO3)2•3H2O and 2,6-pyridine dicarboxylic acid in a 1:1 molar proportion. It has been characterized using FT-IR, XRD, nitrogen adsorption analysis SEM and TEM-EDX. Cu-MOF has anticancer properties against MCF-7 breast cancer cells. Cytotoxicity testing was performed on MCF-7 breast cancer cells using the MTT cell viability assay, and cell proliferation and viability were found to be approximately 24 % higher than the control.

scholarly journals Synthesis and anticancer properties of 5-(1H-benzoimidazol-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids

Pharmacia ◽  
2021 ◽  
Vol 68 (1) ◽  
pp. 195-200
Author(s):  
Volodymyr Horishny ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Combinatorial Library ◽  
Leukemia Cell ◽  
Anticancer Properties ◽  
H Nmr ◽  
Therapeutic Program ◽  
Leukemia Cell Lines ◽  
Cns Cancer

The reaction of 1H-benzoimidazole-2-carbaldehyde with 4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids was studied and the combinatorial library of 5-(1H-benzoimidazol-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-ylcarboxilic acids has been prepared. The structures of target compounds 8a-f, 9 and 10a, b were confirmed by using 1H NMR spectroscopy and elemental analysis. The synthesized compounds were selected by the National Cancer Institute (NCI) Developmental Therapeutic Program for the in vitro cell line screening to investigate their anticancer activity. The tested compounds displayed a weak to medium anticancer activity. The most sensitive cell lines turned out to be SNB-75 of CNS Cancer (GP = 74.84–85.73%) and UO-31, Renal cancer (GP = 71.53–82.16%) and to compound 10a K-562 Leukemia cell lines (GP = 57.14). Graphical abstract

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