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Green Approach Toward Triazole Forming Reactions for Developing Anticancer Drugs.

Shiva K Rastogi1, Veronica C Ciliberto1, Monica Z Trevino1

  • 1Department of Chemistry and Biochemistry, Texas State University, 601 University Drive, San Marcos, TX, 78666, USA.

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Green chemistry approaches are crucial for synthesizing triazole compounds, which exhibit significant anticancer properties. This review highlights recent advancements in eco-friendly click reactions for creating novel triazole-based anticancer agents.

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Area of Science:

  • Medicinal Chemistry
  • Green Chemistry
  • Organic Synthesis

Background:

  • Triazole compounds are vital in pharmaceuticals, dyes, and materials science.
  • They exhibit a broad spectrum of biological activities, including anticancer, antimicrobial, and antioxidant properties.
  • Efficient and environmentally friendly synthesis of triazoles is critical for pharmaceutical development.

Purpose of the Study:

  • To review the last five years of green chemistry approaches for synthesizing 1,2,3-triazole moieties.
  • To focus on the application of these methods in creating biologically active compounds, particularly anticancer agents.
  • To highlight the incorporation of triazoles into natural products and drug-like molecules.

Main Methods:

  • Review of literature focusing on green chemistry principles applied to click reactions (alkyne-azide cycloaddition).
  • Analysis of synthetic strategies for incorporating 1,2,3-triazole rings into diverse molecular scaffolds.
  • Evaluation of cytotoxicity data for synthesized triazole analogues against various cancer cell lines.

Main Results:

  • Several green chemistry methods have been developed for efficient triazole synthesis, reducing hazardous solvent and reagent use.
  • 1,2,3-Triazole moieties were successfully installed in various natural products and synthetic molecules, including colchicine, flavonoids, and bisphosphonates.
  • Many synthesized triazole hybrid analogues demonstrated significant cytotoxicity against a range of cancer cell lines, including multidrug-resistant ones.

Conclusions:

  • Green chemistry approaches significantly enhance the synthesis of triazole-based compounds for pharmaceutical applications.
  • The click reaction provides a versatile route for generating novel triazole hybrids with potent anticancer activities.
  • Further research into eco-friendly triazole synthesis holds great promise for developing new cancer therapeutics.