scholarly journals Synthesis and Evaluation of Triazolyl Dihydropyrimidines as Potential Anticancer Agents

2018 ◽  
Vol 10 (4) ◽  
pp. 18
Author(s):  
Rajanna Ajumeera ◽  
Ganapathi Thipparapu ◽  
Shireesha Boyapati ◽  
Bharath Singh Padya ◽  
Vijayalaxmi Venkatesan
Keyword(s):  
Anticancer Agents ◽  
Human Breast Cancer Cell ◽  
S Phase ◽  
Human Breast ◽  
Standard Drug ◽  
M Phase ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Mcf 7

Novel N – triazolyl 3(a-f) and O-triazolyl (4a-f) derivatives of 4, 6-diaryl-1, 4-dihydropyrimidines were synthesized through mannich reaction. All compounds were characterized by physical and spectral data. These compounds were screened for in vitro efficiency in human breast cancer cell (MCF-7&MDA-MB-231) lines and found to have very good anti-proliferative activity.  Among all compounds of 4b, 3e, 4e endowed with lesser respective IC50 values of 31.94, 55.73, 55.03 µM in MCF-7 cells and 41.50, 35.28, 32.06 µM in MDA-MB 231 cells by MTT assay. In further studies, Compounds 4b, 3e, 4e were found to arrest cell growth at S phase in MCF-7 cells. In MDA-MB 231 cells, 4b, 4e were found to arrest the cells in S phase, and compound 3e found to arrest G2/M phase when compared to the standard drug tamoxifen, arrested S phase in MCF-7 cells and G0/G1 phase in MDA-MB 231 cells.

scholarly journals Synthesis of Novel Chalcone-Based Phenothiazine Derivatives as Antioxidant and Anticancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4566
Author(s):  
Nourah A. Al Zahrani ◽  
Reda M. El-Shishtawy ◽  
Mahmoud M. Elaasser ◽  
Abdullah M. Asiri
Keyword(s):  
Breast Cancer ◽  
Hepatocellular Carcinoma ◽  
Anticancer Agents ◽  
Human Breast Cancer ◽  
Cancer Cell Line ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Phenothiazine Derivatives ◽  
Ic50 Values ◽  
Mcf 7

Based on reported results for the potential medicinal impact of phenothiazine core, as well as the chalcone skeleton that is widely present in many natural products, together with their reported bioactivities, the present work was aimed at combining both moieties in one molecular skeleton and to synthesize and characterize a novel series of chalone-based phenothiazine derivatives. For this purpose, 2-acetylphenothiazine was N-alkylated, followed by the Claisen-Schmidt reaction to produce the chalcones with good yield. Antioxidant activity, as evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, was assessed to determine if their antioxidant potential was comparable with ascorbic acid, and attributable to the phenothiazine core. Screening anticancer activities of the synthesized chalone-based phenothiazine derivatives against human breast cancer cell line MCF-7 cells, and human hepatocellular carcinoma HepG-2 cells, compared with standard drugs cisplatin and doxorubicin, was evaluated. The results revealed that compounds 4a, 4b, 4d, 4h, 4j, 4k, 4m, 4o, and 4p were good against human hepatocellular carcinoma HepG-2 cells, and among these compounds 4b and 4k were the most effective compounds, with IC50 values of 7.14 μg/mL and 7.6 1 μg/mL, respectively. On the other hand, compounds 4a, 4b, 4k, and 4m were good against human breast cancer cell line MCF-7 cells and, among these compounds, 4k and 4b were the most effective compounds, with IC50 values of 12 μg/mL and 13. 8 μg/mL, respectively. The overall results suggest that these compounds could, potentially, be further modified for the formation of more potent antioxidant and anticancer agents.

scholarly journals Homoeopathic Viscum album (10-3) is More Cytotoxic to in vitro Culture of Human Breast Cancer Cell Line than to Human Mesenchymal Stem Cells

2021 ◽  
Vol 19 (4) ◽  
pp. 25-34
Author(s):  
Ana Catarina Viana Valle ◽  
Lana Ribeiro Aguiar ◽  
Hilana dos Santos Sena Brunel ◽  
Patricia Furtado Malard ◽  
Carla Lujan Pereira Villarroel ◽  
...  
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Cell Line ◽  
Culture Medium ◽  
Cancer Cell Line ◽  
Viscum Album ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Mcf 7

BACKGROUND Adenocarcinomas can be of several types, and MCF-7 is an adenocarcinoma of human breast cell line useful as preclinical model to screen therapeutic agents such as ultra-diluted Viscum album, an European plant whose extract is commonly used in cancer therapy. AIMS MCF-7 and mesenchymal stem cells were used to evaluate the in vitro cytotoxicity of homoeopathic Viscum album 1x10-3 (VAD3). METHODS cells were cultured for 24 hours in controlled environment (37.5oC and 5% CO2) in 96-well plates. After this time, VAD3 was added to the culture medium in concentrations varying from 10 to 100 ?L/mL for MTT assay (evaluation of viability of cells). A control group was maintained with culture medium only. After 48 hours, the procedures of analysis of cells viability were performed. RESULTS MTT assay showed that the concentrations of 42 ?L/mL and 62 ?L/mL were able to reduce cell viability to 50% in MCF-7 and mesenchymal stem cells, respectively, which means that half of the cells cultured were dead after 48 hours in contact with VAD3. CONCLUSION Viscum album presented higher cytotoxic action on human breast cancer cell line culture than on mesenchymal stem cells. This medicine is extensively used against cancer, and the use of the homoeopathic form of it brings new possibilities as no or fewer adverse effects would be present.

Diethylenetriamine Pentaacetic Acid Derivative of Toremifene and In Vitro Evaluation in Human Breast Cancer Cell Line MCF-7

2011 ◽  
Vol 26 (1) ◽  
pp. 105-111 ◽  
Author(s):  
Ayfer Yurt Kilcar ◽  
F. Zumrut Biber Muftuler ◽  
Perihan Unak ◽  
Cigir Biray Avci ◽  
Cumhur Gunduz
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Acid Derivative ◽  
Breast Cancer Cell Line ◽  
Human Breast Cancer ◽  
Cancer Cell Line ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Mcf 7

In vitro andin vivo modulation of growth regulation in the human breast cancer cell line MCF-7 by estradiol metabolites

Breast Cancer ◽  
1999 ◽  
Vol 6 (2) ◽  
pp. 87-92 ◽  
Author(s):  
Akihiko Suto ◽  
Nitin T. Telang ◽  
Hirokazu Tanino ◽  
Toshio Takeshita ◽  
Harumi Ohmiya ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Cell Line ◽  
Human Breast Cancer ◽  
Growth Regulation ◽  
Cancer Cell Line ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Estradiol Metabolites ◽  
Mcf 7

Mechanism of apoptotic induction in human breast cancer cell, MCF-7, by an analog of curcumin in comparison with curcumin – An in vitro and in silico approach

2014 ◽  
Vol 210 ◽  
pp. 51-63 ◽  
Author(s):  
Kumaravel Mohankumar ◽  
Sankar Pajaniradje ◽  
Subhashree Sridharan ◽  
Vivek Kumar Singh ◽  
Larance Ronsard ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
In Silico ◽  
Human Breast Cancer ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Apoptotic Induction ◽  
Mcf 7

SYNTHESIS AND EVALUATION OF NOVEL CHEMICAL ENTITIES AS ANTI-BREAST CANCER AGENTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (12) ◽  
pp. 28-31
Author(s):  
D Nikam ◽  
◽  
S. Tanvar ◽  
A Kute ◽  
S Lokhande ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Human Breast Cancer ◽  
Cancer Cell Line ◽  
Aromatic Aldehydes ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Compound I ◽  
Green Method ◽  
Mcf 7

A series of dihydropyrimidone derivatives was synthesized by an efficient, simple and solvent less green method by using Beginelli reaction. Various aromatic aldehydes, urea and ethyl acetoacetate were refluxed for a few hours and the reaction monitored by periodic TLC (hexane: ethyl acetate 6:4 v/v) and products are purified by recrystallization, with characterization by FTIR, 1H NMR. All the purified compounds were subjected to evaluatation by in vitro human breast cancer cell line MDA-MB-231 and MCF-7. Compound I-k was found to be moderately active against MCF-7 with GI 50 value of -4.38.

scholarly journals Chitosan-Coated Halloysite Nanotubes As Vehicle for Controlled Drug Delivery to MCF-7 Cancer Cells In Vitro

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2837
Author(s):  
Emmanuel Nyankson ◽  
Shadrack O. Aboagye ◽  
Johnson Kwame Efavi ◽  
Benjamin Agyei-Tuffour ◽  
Lily Paemka ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Viability ◽  
Breast Cancer Cell ◽  
Human Breast Cancer ◽  
Trypan Blue ◽  
Halloysite Nanotubes ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Mcf 7

The aim of the work is to improve the release properties of curcumin onto human breast cancer cell lines using coated halloysite nanotubes (HNTs) with chitosan as a polycation. A loading efficiency of 70.2% (w/w) was attained for loading 4.9 mg of the drug into 0.204 g bed volume of HNTs using the vacuum suction method. Results acquired from Brunauer-Emmett-Teller (BET), Fourier-transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), scanning electron spectroscopy (SEM), zeta potential, and thermogravimetric analysis (TGA) indicated the presence of the drug and the biopolymer in and around the nanotubes. The release properties of drug-loaded HNTs (DLHNTs) and chitosan-coated drug-loaded HNTs (DLHNTs-CH) were evaluated. The release percentages of DLHNTs and DLHNTs-CH after 6 h were 50.7 and 37%, respectively. Based on the correlation coefficients obtained by fitting the release nature of curcumin from the two samples, the Korsmeyer-Peppas model was found to be the best-fitted model. In vitro cell viability studies were carried out on the human breast cancer cell line MCF-7, using the MTT and trypan blue exclusion assays. Prior to the Trypan blue assay, the IC50 of curcumin was determined to be ~30 µM. After 24 h of incubation, the recorded cell viability values were 94, 68, 57, and 51% for HNTs, DLHNTs-CH, DLHNTs, and curcumin, respectively. In comparison to the release studies, it could be deducted that sustained lethal doses of curcumin were released from the DLHNTs-CH within the same time. It is concluded from this work that the “burst release” of naked drugs could be slowly administered using chitosan-coated HNTs as potential drug carriers.

Sign in / Sign up

Export Citation Format

Share Document