Maryam Gilandoust and Harsha, K. B. and Mohan, C. D. and Raquib, A. R. and Rangappa, S. and Pandey, Vijay and Lobie, Peter E. and Basappa and Rangappa, K. S. (2018) Synthesis, characterization and cytotoxicity studies of 1,2,3-triazoles and 1,2,4-triazolo 1,5-a pyrimidines in human breast cancer cells. Bioorganic & Medicinal Chemistry Letters, 28 (13). 2314 - 2319. ISSN 1464-3405
Full text not available from this repository. (Request a copy)Abstract
Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) is essential for physiological functions of tissues and neovasculature. VEGFR signaling is associated with the progression of pathological angiogenesis in various types of malignancies, making it an attractive therapeutic target in cancer treatment. In the present work, we report the synthesis of 1,4-disubstituted 1,2,3-triazoles and 1,2,4-triazolo1, 5-apyrimidine derivatives via copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction and screened for their anticancer activity against MCF7 cells. We identified 1-(2′-ethoxy-4′-fluoro-1,1′-biphenyl-4-yl)-4-phenyl-1H-1,2,3-triazole (EFT) as lead cytotoxic agent against MCF7 cell lines with an IC50 value of 1.69 µM. Further evaluation revealed that EFT induces cytotoxicity on Ishikawa, MDA-MB-231 and BT474 cells with IC50 values of 1.97, 4.81 and 4.08 µM respectively. However, EFT did not induce cytotoxicity in normal lung epithelial (BEAS-2B) cells. Previous reports suggested that 1,2,3-triazoles are the inhibitors of VEGFR1 and therefore, we evaluated the effect of EFT on the expression of VEGFR1. The results demonstrated that EFT downregulates the expression of VEGFR1 in MCF7 cells. In summary, we identified a potent cytotoxic agent that imparts its antiproliferative activity by targeting VEGFR1 in breast cancer cells. The novel compound could serve as a lead structure in developing VEGFR1 inhibitors.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | 1,2,3-Triazole, 1,2,4-Triazole, Angiogenesis, VEGFR1, Anticancer agent |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Manjula P Library Assistant |
| Date Deposited: | 25 Jul 2019 06:15 |
| Last Modified: | 22 Jun 2022 06:05 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/5544 |
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