Synthesis of Novel Benzofuran Spiro-2-Pyrrolidine Derivatives via [3+2] Azomethine Ylide Cycloadditions and Their Antitumor Activity
2024

New Antitumor Compounds from Benzofuran Derivatives

publication Evidence: moderate

Author Information

Author(s): Pan Bowen, Wang Tao, Zheng Liangliang, Dong Zhangchao, Liu Lijuan, Liu Xiongwei, Feng Tingting, Zhou Ying, Shi Yang, Margetic Davor

Primary Institution: College of Pharmacy, Guizhou University of Traditional Chinese Medicine

Hypothesis

Can novel benzofuran spiro-pyrrolidine derivatives exhibit significant antitumor activity?

Conclusion

The study successfully synthesized 24 benzofuran spiro-pyrrolidine derivatives, some of which showed better antiproliferative activities against cancer cells than cisplatin.

Supporting Evidence

  • Compounds 4b and 4c showed higher antiproliferative activities against HeLa cells than cisplatin.
  • Compounds 4e and 4s exhibited better inhibitory activities against CT26 cells than cisplatin.
  • The reaction produced derivatives with yields ranging from 74% to 99%.

Takeaway

Scientists made new compounds from benzofuran that might help fight cancer better than some current treatments.

Methodology

The compounds were synthesized using a three-component [3+2] azomethine ylide cycloaddition reaction, and their antitumor activities were evaluated using the MTT method.

Limitations

The study does not address the long-term effects or potential side effects of the new compounds.

Digital Object Identifier (DOI)

10.3390/ijms252413580

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