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

被引：10
|
作者：
Kumar, Dinesh [1 ]
Nepali, Kunal [1 ]
Bedi, P. M. S. [1 ]
Kumar, Suresh [2 ]
Malik, Fayaz [2 ]
Jain, Subheet [1 ]
机构：
[1] Guru Nanak Dev Univ, Dept Pharmaceut Sci, Amritsar 143005, Punjab, India
[2] Indian Inst integrat Med, Jammu, India
来源：
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY | 2015年 / 15卷 / 06期
关键词：
Apoptosis; cell cycle; chalcone; contrained; cytotoxic; pyrimidones; BIOLOGICAL EVALUATION; DERIVATIVES;
D O I：
10.2174/1871520615666150318101436
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
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 mu M 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 mu M compound SK-25.
引用
收藏
页码：793 / 803
页数：11
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