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

研究成果: 雜誌貢獻文章

6 引文 斯高帕斯(Scopus)

摘要

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.
原文英語
頁(從 - 到)793-803
頁數11
期刊Anti-Cancer Agents in Medicinal Chemistry
15
發行號6
DOIs
出版狀態已發佈 - 七月 1 2015
對外發佈Yes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

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