We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis and pharmacological evaluation of 2,3‐diphenyl acrylonitriles‐bearing halogen as selective anticancer agents.
- Authors
Li, Jia‐jun; Ma, Jun; Xin, Ya‐bing; Quan, Zhe‐shan; Tian, Yu‐shun
- Abstract
Eighteen novel 2,3‐diphenyl acrylonitrile derivatives bearing halogens were designed, synthesized, and evaluated for biological activity. Preliminary in vitro results indicated that the majority of the compounds with a para‐substituted halogen had considerable antiproliferative activity against five human cancer cell lines, including MGC‐803, AGS, and BEL‐7402, with IC50 values in the range of 0.46–100 μ m. No significant toxic effects on the non‐cancerous human liver cell line L‐02 were observed. The selective inhibitory activities against cancer cells were significantly better than that of the control lead compound CA‐4 and CA‐4P. Particularly, potent activities were found for the derivatives of 3‐(4‐halogen phenyl)‐2‐(3,4,5‐trimethoxyphenyl)acrylonitrile, such as 5c (4‐fluoro), 5f (4‐bromo), 5h (4‐chloro), and 5k (4‐trifluoro‐ methyl), for AGS with IC50 values of 0.75 ± 0.24, 0.68 ± 0.21, 0.41 ± 0.05, and 1.49 ± 0.92 μ m, respectively. The antiproliferative effects of 5f were attributed to cell‐cycle arrest in the G2/M phase, induction of cellular apoptosis, suppression of cell migration, and inhibition of cell colony formation in AGS cells.
- Subjects
ACRYLONITRILE analysis; ANTINEOPLASTIC agent synthesis; HALOGEN compounds; DRUG design; CANCER cells
- Publication
Chemical Biology & Drug Design, 2018, Vol 92, Issue 2, p1419
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13180