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Volume 21, Issue 16
  • ISSN: 1570-1808
  • E-ISSN: 1875-628X

Abstract

Background

Thirteen derivatives were designed and synthesized based on the excellent lead compound Matrine.

Objective

This study aimed to discover novel anticancer agents with superior anticancer activity and to support the discovery of new drugs.

Methods

The antiproliferative activity of all derivatives against four human cancer cells, A549, HGC-27, HCT-116, and HeLa, was determined by MTT. The best active compounds were subjected to cell cloning, migration, cell cycle and apoptosis, and molecular docking.

Results

Compound showed the best activity against all four cell lines, especially against A549 cells, with an IC of 5.805 μmol/L. The antiproliferative activity of was much higher than that of matrine and only slightly weaker than that of Cisplatin, a multi-targeted small molecule inhibitor. also showed excellent inhibitory activity in cell cycle, apoptosis, cell scratch, and cell cloning assays and has shown good affinity in docking studies.

Conclusion

has excellent antiproliferative activity, significantly inhibits cell cloning and migration, affects cancer cell cycle distribution, and induces apoptosis in a concentration-dependent manner, making it a potential anticancer drug agent.

© 2024 Bentham Science Publishers
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2024-04-15
2024-12-23

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Design, Synthesis, and In vitro Biological Activities of Matrine Skeleton Derivatives as Potential Cancer Inhibitors
Letters in Drug Design & Discovery 21, 3590 (2024); https://doi.org/10.2174/0115701808300981240408063655
/content/journals/lddd/10.2174/0115701808300981240408063655
/content/journals/lddd/10.2174/0115701808300981240408063655
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  • Article Type:     Research Article
Keyword(s): anticancer agents; antiproliferative; imidazo[2,1-b]thiazole; Matrine; synthesis; thiazole

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