Semicarbazone Derivatives Bearing Phenyl Moiety: Synthesis, Anticancer Activity, Cell Cycle, Apoptosis-Inducing and

Junjie Ma1, Xin Ni1, Yali Gao2

  • 1Medical College, Huaqiao University.

Insights

New semicarbazone derivatives, 11q and 11s, demonstrate potent anticancer activity against multiple human cancer cell lines. These compounds induce apoptosis and cell cycle arrest, showing promise as novel cancer therapeutics with low toxicity to normal cells.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Semicarbazone derivatives are explored for their therapeutic potential.
  • Developing novel anticancer agents with improved efficacy and safety is crucial.

Purpose of the Study:

  • To synthesize and evaluate novel semicarbazone derivatives for anticancer activity.
  • To identify lead compounds for further cancer drug development.

Main Methods:

  • Synthesis of phenyl-bearing semicarbazone derivatives.
  • In vitro anticancer screening against human cancer cell lines (HT29, SK-N-SH, MDA-MB-231, MKN45).
  • Flow cytometry for cell cycle and apoptosis analysis, enzymatic assays, and metabolic stability studies.

Main Results:

  • Compounds 11q and 11s exhibited potent in vitro anticancer activity (IC50: 0.32–1.57 µM) against tested cancer cells.
  • 11q and 11s showed weak cytotoxicity against normal human umbilical vein endothelial cells (HUVEC).
  • These compounds induced Sub-G1 cell cycle arrest and apoptosis, activating caspase-3, with moderate metabolic stability.

Conclusions:

  • 11q and 11s are identified as promising lead compounds for anticancer drug development.
  • The mechanism involves apoptosis induction and cell cycle arrest.
  • Further preclinical development is warranted based on potent activity and favorable preliminary safety profile.

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