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Design, synthesis and cytotoxicity of chimeric erlotinib-alkylphospholipid hybrids

Md Maqusood Alam1, Ahmed H E Hassan2, Kun Won Lee1

  • 1Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Republic of Korea.

Bioorganic Chemistry
|November 28, 2018
PubMed

Insights

New erlotinib-alkylphospholipid hybrids show potent anticancer activity. Amide derivatives demonstrated superior antiproliferative effects against lung, breast, liver, and skin cancer cells compared to existing treatments.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Pharmacology

Background:

  • Erlotinib is a targeted therapy for certain cancers.
  • Alkylphospholipids have shown anticancer properties.
  • Developing novel hybrid molecules can enhance therapeutic efficacy.

Purpose of the Study:

  • To synthesize and evaluate novel erlotinib-alkylphospholipid hybrids.
  • To assess the antiproliferative activity of these hybrids against various cancer cell lines.
  • To compare the efficacy of amide and ester analogs.

Main Methods:

  • Synthesis of two series of erlotinib-alkylphospholipid hybrids (amide and ester analogs).
  • Evaluation of antiproliferative activity using cell viability assays (GI50 values).
  • Assays for EGFR kinase and Akt phosphorylation inhibition, coupled with statistical correlation analysis.

Main Results:

  • Amide analogs exhibited enhanced cytotoxic activity compared to ester analogs.
  • Derivatives 8d and 8e showed broad-spectrum antiproliferative activity with high efficacy.
  • Cellular GI50 values for 8d and 8e were in the low micromolar range.
  • Correlation analysis suggested potential alternative mechanisms of action for amide derivatives.

Conclusions:

  • Erlotinib-alkylphospholipid amide hybrids represent promising anticancer agents.
  • These hybrids display superior efficacy over erlotinib and miltefosine.
  • The cytotoxic mechanisms may vary between amide and ester series and across different cancer cell types.
Keywords:
Akt phosphorylationAlkylphospholipids (APL)Epidermal growth factor receptor (EGFR)Erlotinib

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