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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts

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Anticancer activity of new coumarin substituted hydrazide-hydrazone derivatives

Tamer Nasr1, Samir Bondock2, Mahmoud Youns3

  • 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Helwan, Egypt.

European Journal of Medicinal Chemistry
|March 11, 2014
PubMed

Insights

Novel coumarin derivatives combat drug-resistant cancer. Compound 7c shows potent anticancer activity by inducing apoptosis and cell cycle arrest in resistant pancreatic cancer cells, offering hope for improved patient outcomes.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Pharmacology

Background:

  • Drug resistance is a significant challenge in cancer therapy.
  • Developing novel agents to overcome resistance is crucial.

Purpose of the Study:

  • To design and synthesize novel coumarin hydrazide-hydrazone derivatives.
  • To evaluate their efficacy against drug-resistant and drug-sensitive cancer cell lines.
  • To investigate their mechanism of action.

Main Methods:

  • Synthesis of sixteen coumarin hydrazide-hydrazone derivatives.
  • In vitro evaluation against human pancreatic (Panc-1), hepatic (Hep-G2), and leukemia (CCRF) cell lines.
  • Assays for cytotoxicity, caspase-3/7 activation, apoptosis induction, and gene expression (microarray).

Main Results:

  • 6-Brominated coumarin hydrazide-hydrazone derivatives (BCHHDs) 7c, 8c, and 10c demonstrated superior potency against resistant Panc-1 cells compared to doxorubicin.
  • BCHHD 7c exhibited significant cytotoxicity across all tested cell lines (IC50: 3.60–6.50 μM).
  • BCHHDs activated caspases 3/7, induced apoptosis in Panc-1 cells, and modulated key genes involved in apoptosis and cell cycle arrest (G2/M).

Conclusions:

  • BCHHD 7c is a potent anticancer agent effective against drug-resistant cancer.
  • The compound induces apoptosis and cell cycle arrest, highlighting its therapeutic potential.
  • 7c may offer a promising strategy to overcome drug resistance in clinical cancer treatment.
Keywords:
AntiproliferativeApoptosisCaspases 3/7CoumarinHydrazide–hydrazoneMicroarray

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