Synthesis and Biological Evaluation of New 1,2,3-Triazole Derivatives of the Chrysin Flavonoid as Anticancer Agents

Author(s):

Venkatagiri Noole, Thotla Krishna, Sudhakar Godeshala, Seyedehmelika Meraji, Kaushal Rege, Chepyala K. Reddy* and Bhavani Kedika*   Pages 160 - 168 ( 9 )

Abstract:

Background and Objective: Chrysin and its derivatives proved to possess potential anti-tumour activity. <p> Materials and Methods: A new series of chrysin analogs containing 1,2,3-triazoles with different substituent groups (5a-5l) was designed, synthesized, and evaluated as potential anticancer agents. The synthesized compounds were characterized using FT-IR, 1H NMR 13C NMR spectroscopy and mass spectrometry. <p> Results: The anticancer activities of the synthesized compounds were studied in four cancer cell lines viz. PC3, PC3-PSMA, MCF-7 and UM-UC-3 using doxorubicin as standard. Among all the tested compounds, 5c was found as most active with IC50 value of 10.8 ± 0.04 μM in PC3 cells and 20.53 ± 0.21 μMin MCF-7 cells, respectively. Flow cytometry analyses indicated that synthesized compounds 5a, 5c, and 5h arrested MCF-7 cells at the G2/M phase in a dose-dependent manner. <p> Conclusion: Chyrsin derivatives could be novel anticancer agents.

Keywords:

Chrysin, triazoles, anticancer activity, drug design, QSAR, cell cycle analysis.

Affiliation:

Department of Chemistry, Osmania University, Hyderabad - 500007, Telangana, Department of Chemistry, Osmania University, Hyderabad - 500007, Telangana, Chemical Engineering, Arizona State University, Tempe, AZ 85287-6106, Chemical Engineering, Arizona State University, Tempe, AZ 85287-6106, Chemical Engineering, Arizona State University, Tempe, AZ 85287-6106, Department of Chemistry, Osmania University, Hyderabad - 500007, Telangana, Department of Chemistry, Osmania University, Hyderabad - 500007, Telangana

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