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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
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Design, Synthesis, and Biological Evaluation of New Potential Unusual Modified Anticancer Immunomodulators for

Reda R Mabrouk1,2, Abdallah E Abdallah1, Hazem A Mahdy1

  • 1Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt.

International Journal of Molecular Sciences
|August 12, 2023
PubMed

Insights

Sixteen new thalidomide analogs show potent anticancer activity against liver, prostate, and breast cancer cells. Compounds XIIIa and XIVc demonstrate significant potential as novel drug candidates for cancer therapy.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Thalidomide analogs are investigated for anticancer properties.
  • Existing cancer therapies require novel drug candidates with improved efficacy.

Purpose of the Study:

  • To synthesize and evaluate novel thalidomide analogs for antiproliferative activity.
  • To identify potent anticancer agents for further drug development.

Main Methods:

  • Synthesis of sixteen new thalidomide analogs.
  • In vitro antiproliferative assays against HepG-2, PC3, and MCF-7 cancer cell lines.
  • Analysis of IC50 values, NFκB P65, caspase-8, TNF-α, and VEGF levels.

Main Results:

  • Several analogs exhibited potent in vitro antiproliferative activities, outperforming thalidomide.
  • Compound XIIIa showed the highest potency with low IC50 values across tested cell lines.
  • Compound XIVc demonstrated significant reduction in NFκB P65, increased caspase-8, and decreased TNF-α and VEGF levels, inducing apoptosis and cell cycle arrest.

Conclusions:

  • The synthesized thalidomide analogs, particularly XIIIa and XIVc, are promising anticancer candidates.
  • Further evaluation of these compounds is warranted for the development of new anticancer drugs.
Keywords:
CRBNimmunomodulatoryquinazolinethalidomide

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