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Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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  1. Home
  3. Design, Synthesis, And In Vitro And In Vivo Biological Evaluation Of 2-amino-naphtho[2,3-b]thiophene-4,9-dione Derivatives As Potent Anticancer Agents.
  1. Home
  3. Design, Synthesis, And In Vitro And In Vivo Biological Evaluation Of 2-amino-naphtho[2,3-b]thiophene-4,9-dione Derivatives As Potent Anticancer Agents.

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Design, synthesis, and in vitro and in vivo biological evaluation of 2-amino-naphtho[2,3-b]thiophene-4,9-dione

Soumen K Manik1, Satyajit Haldar2, Ankita Bhattachrya3

  • 1Department of Chemistry, Coastal Environmental Studies Research Centre, Egra Sarada Shashi Bhusan College, Vidyasagar University, Egra, Purba Medinipur, West Bengal, 721429, India.

European Journal of Medicinal Chemistry
|June 14, 2025

View abstract on PubMed

Summary
This summary is machine-generated.

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A novel compound, 4a, shows potent anticancer effects against triple-negative breast cancer (TNBC) by inducing apoptosis and inhibiting the Akt pathway. This selective targeting offers a promising therapeutic strategy for TNBC treatment.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Molecular Biology

Background:

  • Triple-negative breast cancer (TNBC) is an aggressive subtype with limited targeted therapies.
  • The PI3K/Akt signaling pathway is frequently dysregulated in TNBC, promoting cancer cell survival.
  • Novel therapeutic agents targeting key pathways in TNBC are urgently needed.

Purpose of the Study:

  • To synthesize and evaluate novel 2-amino-naphtho[2,3-b]thiophene-4,9-dione derivatives as potential anticancer agents.
  • To investigate the anticancer mechanisms of the lead compound, 4a, against TNBC cells.
  • To assess the compound's selectivity and potential for targeted therapy.

Main Methods:

  • Multi-component reactions utilizing Domino and Krapcho strategies for synthesis.
  • In vitro evaluation of anticancer activity using MDA-MB-231 (TNBC) cell line.
  • Cell viability, cell cycle, apoptosis, and Western blot analyses to elucidate mechanisms.
  • Immunocytochemistry to assess Akt phosphorylation status.

    • Main Results:

    • Fifteen derivatives were synthesized, with compound 4a exhibiting potent activity against MDA-MB-231 cells.
    • Compound 4a induced dose-dependent inhibition of cell viability, cell cycle arrest, and apoptosis.
    • Apoptosis was mediated by increased caspase-3/7 activation and reactive oxygen species (ROS) generation.
    • Compound 4a significantly suppressed Akt phosphorylation at Ser473, disrupting pro-survival signaling.

    Conclusions:

    • Compound 4a is a promising lead compound for TNBC therapy.
    • The anticancer effects are attributed to the induction of apoptosis and selective inhibition of the Akt pathway.
    • Compound 4a demonstrates potential as a targeted therapeutic agent for TNBC, sparing normal cells.