New synthetic compounds kill colon cancer cells via multiple mechanisms including HDAC inhibition.

New sulfonamide-Schiff base compounds (3a-d) showed significant anticancer activity against DLD-1 and HT-29 CRC cell lines with no toxicity to normal CCD-18Co cells. Compound 3c was most potent in DLD-1 (IC50=3.94 µM) and 3b in HT-29 (IC50=3.26 µM). Multi-mechanism activity: apoptosis induction,…

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New synthetic compounds kill colon cancer cells via multiple mechanisms including HDAC inhibition.

New synthetic compounds kill colon cancer cells via multiple mechanisms including HDAC inhibition.

New sulfonamide-Schiff base compounds (3a-d) showed significant anticancer activity against DLD-1 and HT-29 CRC cell lines with no toxicity to normal CCD-18Co cells. Compound 3c was most potent in DLD-1 (IC50=3.94 µM) and 3b in HT-29 (IC50=3.26 µM). Multi-mechanism activity: apoptosis induction, HDAC inhibition (3d: 69% in HT-29), antioxidant induction, and p38/MAPK activation.

Key Findings

  • Compound 3c IC50=3.94 µM in DLD-1; compound 3b IC50=3.26 µM in HT-29
  • No toxicity to normal CCD-18Co colon cells
  • Multi-mechanism activity: apoptosis, HDAC inhibition, antioxidant effects, p38/MAPK activation
  • Compound 3d: 69% HDAC inhibition in HT-29 cells
  • p38/MAPK activation and ERK1 downregulation as key signaling mechanism

Implications

Multi-mechanism activity profile makes these early-stage candidates interesting for CRC drug development. HDAC inhibitory activity is notably valuable.

Caveats

In vitro cell line study; abstract-only. Results require in vivo validation. Multi-mechanism activity may create off-target effects in vivo.

Source: Archiv der Pharmazie — 2026-04-01

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