Abstract
A Series of chalcone derivatives containing pyrazole ring was prepared and their cytotoxicity against different human cell lines, including breast (MCF-7), colon (HCT-116) liver (HEPG2) cell lines, as well as normal melanocyte HFB4 was evaluated. Two of these chalcone derivatives with different IC50 and chemical configuration were chosen for molecular studies in detail with MCF-7 cells. Our data indicated that the two compounds prohibit proliferation, angiogenesis, cell cycle progression and induce apoptosis of breast cancer cells. This inhibition is mediated by up regulation of tumor suppressor p53 associated with arrest in S-G2/M of cell cycle. This work provides a confirmation of antitumor activity of the novel chalcones and assists the development of new agents for cancer treatment.
Keywords: Angiogenesis, Apoptosis, Breast carcinoma cell line MCF-7, Caspases, Cell cycle arrest, Chalcones, P53.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:Chalcones Incorporated Pyrazole Ring Inhibit Proliferation, Cell Cycle Progression, Angiogenesis and Induce Apoptosis of MCF7 Cell Line
Volume: 14 Issue: 9
Author(s): Magda F. Mohamed, Mervat S. Mohamed, Mohamed M. Fathi, Samia A. Shouman and Ismail Abdelshafy Abdelhamid
Affiliation:
Keywords: Angiogenesis, Apoptosis, Breast carcinoma cell line MCF-7, Caspases, Cell cycle arrest, Chalcones, P53.
Abstract: A Series of chalcone derivatives containing pyrazole ring was prepared and their cytotoxicity against different human cell lines, including breast (MCF-7), colon (HCT-116) liver (HEPG2) cell lines, as well as normal melanocyte HFB4 was evaluated. Two of these chalcone derivatives with different IC50 and chemical configuration were chosen for molecular studies in detail with MCF-7 cells. Our data indicated that the two compounds prohibit proliferation, angiogenesis, cell cycle progression and induce apoptosis of breast cancer cells. This inhibition is mediated by up regulation of tumor suppressor p53 associated with arrest in S-G2/M of cell cycle. This work provides a confirmation of antitumor activity of the novel chalcones and assists the development of new agents for cancer treatment.
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Mohamed F. Magda, Mohamed S. Mervat, Fathi M. Mohamed, Shouman A. Samia and Abdelhamid Abdelshafy Ismail, Chalcones Incorporated Pyrazole Ring Inhibit Proliferation, Cell Cycle Progression, Angiogenesis and Induce Apoptosis of MCF7 Cell Line, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (9) . https://dx.doi.org/10.2174/187152061409141010114547
DOI https://dx.doi.org/10.2174/187152061409141010114547 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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