Design, Synthesis and Anti-breast Cancer Activity of Some Novel Substituted Isoxazoles as Anti-breast Cancer Agent

2018 ◽  
Vol 18 (7) ◽  
pp. 1009-1015
Author(s):  
Santosh N. Mokale ◽  
Nikhil S. Sakle ◽  
Swati A. Bhavale ◽  
Deepak K. Lokwani ◽  
Vishakha R. Shelke

Methods: A novel series of isoxazole (S21-S30) derivatives were designed, synthesized and screened for their anticancer activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. The synthesized derivative has the ability to inhibit the growth of the human breast cancer cell line at low concentrations. In vivo anticancer activity was performed on virgin female sprague dawley rats. Results: The result shows that compound S23 has more selectivity and marked estrogen modulator activity than the standard tamoxifen.

2019 ◽  
Vol 19 (10) ◽  
pp. 1253-1261 ◽  
Author(s):  
Naipeng Cui ◽  
Dan-Dan Lin ◽  
Yang Shen ◽  
Jian-Guo Shi ◽  
Bing Wang ◽  
...  

Background: Coumarins are a wide group of naturally occurring compounds which exhibit a wide range of biological properties such as anti-cancer activities. Here, we characterized the biological functions of three Triphenylethylene-Coumarin Hybrids (TCHs) both in cell culture and nude mouse model. Methods: Cell proliferation assay was performed in the cell cultures of both EA.hy926 endothelial cell and breast cancer cell lines treated with different concentrations of compound TCH-10b, TCH-5a and TCH-5c. Flowcytometry assay and Western blotting were used to further investigate the effect and mechanism of TCH-5c on EA.hy926 cell proliferation and cell cycle. The effects of TCH-5c on endothelial cell migration and angiogenesis were determined using cytoskeleton staining, migration assay and tube formation assay. Inhibition of breast cancer cell line derived VEGF by TCH-5c was shown through ELISA and the use of conditioned media. SK-BR-3 xenograft mouse model was established to further study the anti-tumorigenic role of compound TCH-5c in vivo. Results: We found that compound TCH-5c has inhibitory effects on both vascular endothelial cells and breast cancer cell lines. Compound TCH-5c inhibited proliferation, resulted in cell death, increased p21 protein expression to induce G0/G1 arrest and changed endothelial cell cytoskeleton organization and migration in EA.hy926 endothelial cells. Compound TCH-5c also inhibited breast cancer cell line derived VEGF secretion, decreased breast cancer cell-induced endothelial cell tube formation in vitro and suppressed SK-BR-3 breast cancer cell-initiated tumor formation in vivo. Conclusion: Our study demonstrates that the coumarin derivative TCH-5c exerts its anti-cancer effects by 1. inhibiting endothelial cell proliferation, migration. 2. suppressing tube formation and angiogenesis induced by breast cancer cells in vitro and in vivo. Our results have potential implications in developing new approaches against breast cancer.


RSC Advances ◽  
2016 ◽  
Vol 6 (103) ◽  
pp. 101415-101429 ◽  
Author(s):  
Pooja Ghosh ◽  
Sudipta Bag ◽  
Atanu Singha Roy ◽  
Elavarasan Subramani ◽  
Koel Chaudhury ◽  
...  

Mor-HSA-NPs and EC-HSA-NPs are effective on MDA-MB-468 breast cancer cell lines.


Molekul ◽  
2020 ◽  
Vol 15 (1) ◽  
pp. 34
Author(s):  
Retno Aliyatul Fikroh ◽  
Sabirin Matsjeh ◽  
Chairil Anwar

Breast cancer is one of cancer causes of death in woman. Chemotherapy is one cancer treatment give toxic effects on normal cells. Alternative of cancer treatment by using flavonoid derivative have potent anticancer to reduce side effects of cancer. Chalcone is family of flavonoid that have biological activity. Chalcone derivatives have potential compound as anticancer agent. Chalcone with the presence halogen, metoxy group in ring B is know to inhibit cancer cells. The aims of this research were to synthesize chalcone derivate with bromo, methoxy, and hyroxy group in ring chalcone and to determine the anticancer activity of chalcone derivative. The chalcone derivative was synthesized from 2-hydroxyacetophenone with 2-bromo-4,5-dimethoxybenzaldehyde by Claisen-Schmidt reaction. In vitro cytotoxicity against breast cancer cell was tested by MTT assay method. The compound of 2’-hydroxy-2-bromo-4,5-dimethoxychalcone was yield in 78% as yellow solid. The IC50 of 2’-hydroxy-2-bromo-4,5-dimethoxychalcone was 42,19 µg/mL as a moderate activity to inhibiting breast cancer cell line. Cytotoxity of docorubicin againts breast cancer cell line more active than 2’-hydroxy-2-bromo-4,5-dimethoxychalcone with IC50 10,61 µg/mL. Doxorubicin as drug standar had better anticancer activity than 2’-hydroxy-2-bromo-4,5-dimethoxychalcone. Based on the IC50 value, the compound 2’-hydroxy-2-bromo-4,5-dimethoxychalcone has a moderate activity towards breast cancer cell lines. This study can recommend as candidate for anticancer againts breast cancer cell lines.


2014 ◽  
Vol 8 (Suppl 4) ◽  
pp. P22
Author(s):  
Klesia Madeira ◽  
Murilo Cerri ◽  
Renata Daltoé ◽  
Alice Herlinger ◽  
João Filho ◽  
...  

Antioxidants ◽  
2019 ◽  
Vol 8 (12) ◽  
pp. 625 ◽  
Author(s):  
Yi-Fen Chiang ◽  
Hsin-Yuan Chen ◽  
Ko-Chieh Huang ◽  
Po-Han Lin ◽  
Shih-Min Hsia

Excessive growth of cancer cells is the main cause of cancer mortality. Therefore, discovering how to inhibit cancer growth is an important research topic. Recently, the newly discovered adipokine, known as nicotinamide phosphoribosyl transferase (NAMPT, visfatin), which has been associated with metabolic syndrome and obesity, has also been found to be a major cause of cancer proliferation. Therefore, inhibition of NAMPT and reduction of Nicotinamide adenine dinucleotide (NAD) synthesis is one strategy for cancer therapy. Cinnamaldehyde (CA), as an antioxidant and anticancer natural compound, may have the ability to inhibit visfatin. The breast cancer cell line and xenograft animal models were treated under different dosages of visfatin combined with CA and FK866 (a visfatin inhibitor) to test for cell toxicity, as well as inhibition of tumor-related proliferation of protein expression. In the breast cancer cell and the xenograft animal model, visfatin significantly increased proliferation-related protein expression, but combination with CA or FK866 significantly reduced visfatin-induced carcinogenic effects. For the first time, a natural compound inhibiting extracellular and intracellular NAMPT has been demonstrated. We hope that, in the future, this can be used as a potential anticancer compound and provide further directions for research.


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