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Synthesis of New Thiazole-Privileged Chalcones as Tubulin Polymerization Inhibitors with Potential Anticancer Activities

Pharmaceuticals, ISSN: 1424-8247, Vol: 17, Issue: 9
2024
  • 3
    Citations
  • 0
    Usage
  • 8
    Captures
  • 2
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    3
  • Captures
    8
  • Mentions
    2
    • Blog Mentions
      1
      • Blog
        1
    • News Mentions
      1
      • News
        1

Most Recent News

Sohag University Researcher Updates Understanding of Anticancer Agents (Synthesis of New Thiazole-Privileged Chalcones as Tubulin Polymerization Inhibitors with Potential Anticancer Activities)

2024 SEP 20 (NewsRx) -- By a News Reporter-Staff News Editor at Cancer Daily -- A new study on anticancer agents is now available. According

Article Description

A series of novel thiazole-based chalcones were evaluated for their anticancer activity as potential tubulin polymerization inhibitors. In vitro anticancer screening for the thiazole derivatives 2a–2p exhibited broad-spectrum antitumor activity against various cancer cell lines particularly Ovar-3 and MDA-MB-468 cells with a GI range from 1.55 to 2.95 μΜ, respectively. Compound 2e demonstrated significant inhibition of tubulin polymerization, with an IC value of 7.78 μM compared to Combretastatin-A4 (CA-4), with an IC value of 4.93 μM. Molecular docking studies of compounds 2e, 2g, and 2h into tubulin further supported these findings, revealing that they bind effectively to the colchicine binding site, mirroring key interactions exhibited by CA-4. Computational predictions suggested favorable oral bioavailability and drug-likeness for these compounds, highlighting their potential for further development as chemotherapeutic agents.

Bibliographic Details

Hashem, Hamada; Hassan, Abdelfattah; Abdelmagid, Walid M; Habib, Ahmed G K; Abdel-Aal, Mohamed A A; Elshamsy, Ali M; El Zawily, Amr; Radwan, Ibrahim Taha; Bräse, Stefan; Abdel-Samea, Ahmed S; Rabea, Safwat M

MDPI AG

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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