New Chalcone Incorporated Structurally Modified Pyridine-Pyrimidine Derivatives as Anticancer Agents: Their Design, Synthesis, and in-vitro Evaluation

Chem Biodivers. 2024 Dec;21(12):e202401122. doi: 10.1002/cbdv.202401122. Epub 2024 Oct 22.

Abstract

Chalcone-incorporated pyridine-pyrimidines i.e. derivatives of (5-(6-(pyrimidin-5-yl)pyridin-3-yl)thiophen-2-yl)prop-2-en-1-one were synthesized and their structures were confirmed by analytical techniques. In addition, all the derivatives were examined for their capacity to fight against cancer towards four cell lines, including breast (MCF-7), prostate (DU-145 and PC3), and lung (A549) by utilizing the MTT technique and the clinically used chemotherapy medication, etoposide serving as a positive reference. All these results were expressed in IC50 μM, and values of synthesized compounds are compared with a reference drug, showing values ranging from 1.97±0.45 μM to 3.08±0.135 μM. Among those, a few compounds 10(a-e) demonstrated strong activities with corresponding cell lines.

Keywords: MTT assay; anticancer activity and in vitro evaluation; chalcone; pyridine-pyrimidines.

MeSH terms

  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation* / drug effects
  • Cell Survival / drug effects
  • Chalcone / chemical synthesis
  • Chalcone / chemistry
  • Chalcone / pharmacology
  • Chalcones / chemical synthesis
  • Chalcones / chemistry
  • Chalcones / pharmacology
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Screening Assays, Antitumor*
  • Humans
  • Molecular Structure
  • Pyridines* / chemical synthesis
  • Pyridines* / chemistry
  • Pyridines* / pharmacology
  • Pyrimidines* / chemical synthesis
  • Pyrimidines* / chemistry
  • Pyrimidines* / pharmacology
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyridines
  • Pyrimidines
  • Chalcone
  • Chalcones