4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents



Anti-Cancer Agents in Medicinal Chemistry, 15(6): 793-803.

Author(s): Dinesh Kumar, Kunal Nepali, PMS Bedi, Suresh Kumar, Fayaz Malik and Subheet Jain.

Affiliation: Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab-143005.

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.




Keywords:

Apoptosis, cell cycle, chalcone, contrained, cytotoxic, pyrimidones.



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Article Details

Volume: 15
Issue Number: 6
First Page: 793
Last Page: 803
Page Count: 11
DOI: 10.2174/1871520615666150318101436
Price: $58
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