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

Venkatagiri Noole, Thotla Krishna, Sudhakar Godeshala, Seyedehmelika Meraji, Kaushal Rege, Chepyala K. Reddy, Bhavani Kedika

Research output: Contribution to journalArticlepeer-review

Abstract

Background and Objective: Chrysin and its derivatives proved to possess potential anti-tumour activity. 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,1 H NMR13 C NMR spectroscopy and mass spectrometry. 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. Conclusion: Chyrsin derivatives could be novel anticancer agents.

Original languageEnglish (US)
Pages (from-to)160-168
Number of pages9
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume22
Issue number1
DOIs
StatePublished - Jan 2022

Keywords

  • Anticancer activity
  • Cell cycle analysis
  • Chrysin
  • Drug design
  • QSAR
  • Triazoles

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

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