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Facile Synthesis of Some Coumarin Derivatives and Their Cytotoxicity through VEGFR2 and Topoisomerase II Inhibition

Molecules, ISSN: 1420-3049, Vol: 27, Issue: 23
2022
  • 10
    Citations
  • 0
    Usage
  • 7
    Captures
  • 1
    Mentions
  • 5
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    10
  • Captures
    7
  • Mentions
    1
    • News Mentions
      1
      • News
        1
  • Social Media
    5
    • Shares, Likes & Comments
      5
      • Facebook
        5

Most Recent News

Findings from Imam Abdulrahman Bin Faisal University in Enzymes and Coenzymes Reported (Facile Synthesis of Some Coumarin Derivatives and Their Cytotoxicity through VEGFR2 and Topoisomerase II Inhibition)

2022 DEC 23 (NewsRx) -- By a News Reporter-Staff News Editor at Cancer Daily -- Current study results on enzymes and coenzymes have been published.

Article Description

Novel semisynthetic coumarin derivatives were synthesized to be developed as chemotherapeutic anticancer agents through topoisomerase II, VEGFR2 inhibition that leads to apoptotic cancer cell death. The coumarin amino acids and dipeptides derivatives were prepared by the reaction of coumarin-3-carboxylic acid with amino acid methyl esters following the N,N-dicyclohexylcarbodiimide (DCC) method and 1-hydroxy-benzotriazole (HOBt), as coupling reagents. The synthesized compounds were screened towards VEGFR2, and topoisomerase IIα proteins to highlight their binding affinities and virtual mechanism of binding. Interestingly, compounds 4k (Tyr) and 6c (β-Ala-L-Met) shared the activity towards the three proteins by forming the same interactions with the key amino acids, such as the co-crystallized ligands. Both compounds 4k and 6c exhibited potent cytotoxic activities against MCF-7 cells with IC values of 4.98 and 5.85 µM, respectively causing cell death by 97.82 and 97.35%, respectively. Validating the molecular docking studies, both compounds demonstrated promising VEGFR-2 inhibition with IC values of 23.6 and 34.2 µM, compared to Sorafenib (30 µM) and topoisomerase-II inhibition with IC values of 4.1 and 8.6 µM compared to Doxorubicin (9.65 µM). Hence, these two promising compounds could be further tested as effective and selective target-oriented active agents against cancer.

Bibliographic Details

Gomaa, Mohamed S; Ali, Ibrahim A I; El Enany, Gaber; El Ashry, El Sayed H; El Rayes, Samir M; Fathalla, Walid; Ahmed, Abdulghany H A; Abubshait, Samar A; Abubshait, Haya A; Nafie, Mohamed S

MDPI AG

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

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