4,6-diaryl pyrimidones as constrained chalcone analogues

Design, synthesis and evaluation as antiproliferative agents

Dinesh Kumar, Kunal Nepali, P. M.S. Bedi, Suresh Kumar, Fayaz Malik, Subheet Jain

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

4,6-diarylpyrimidones as constrained chalcone analogues have been synthesised in the present study. The synthesised compounds were evaluated against a panel of human cancer cell lines. Striking selectivity was displayed by the compounds against MiaPaCa (Pancreatic) cell lines while PC-3 (prostate) and A-549 (lung) cell lines were almost resistant to the exposure of the test compounds. Compound SK – 25 exhibited remarkable cytotoxicity against MiaPaca-2 cell line with an IC50 value of 1.95 μM and was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining and mitochondrial membrane potential loss. The cell phase distribution studies indicated that the apoptotic population increased from 1.79% in control sample to 30.33 % in sample treated with 20 μM compound SK-25.

Original languageEnglish
Pages (from-to)793-803
Number of pages11
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume15
Issue number6
DOIs
Publication statusPublished - Jul 1 2015
Externally publishedYes

Fingerprint

Pyrimidinones
Chalcone
Cell Line
Phase-Contrast Microscopy
Mitochondrial Membrane Potential
Inhibitory Concentration 50
Prostate
Apoptosis
Staining and Labeling
Lung
Population
Neoplasms

Keywords

  • Apoptosis
  • Cell cycle
  • Chalcone
  • Contrained
  • Cytotoxic
  • Pyrimidones

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

Cite this

4,6-diaryl pyrimidones as constrained chalcone analogues : Design, synthesis and evaluation as antiproliferative agents. / Kumar, Dinesh; Nepali, Kunal; Bedi, P. M.S.; Kumar, Suresh; Malik, Fayaz; Jain, Subheet.

In: Anti-Cancer Agents in Medicinal Chemistry, Vol. 15, No. 6, 01.07.2015, p. 793-803.

Research output: Contribution to journalArticle

Kumar, Dinesh ; Nepali, Kunal ; Bedi, P. M.S. ; Kumar, Suresh ; Malik, Fayaz ; Jain, Subheet. / 4,6-diaryl pyrimidones as constrained chalcone analogues : Design, synthesis and evaluation as antiproliferative agents. In: Anti-Cancer Agents in Medicinal Chemistry. 2015 ; Vol. 15, No. 6. pp. 793-803.
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