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KMID : 1059520200640010007
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Journal of the Korean Chemical Society
2020 Volume.64 No. 1 p.7 ~ p.18
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Synthesis and Antiproliferative Potency within Anticonvulsant of Novel Bichalcone Derivatives
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Mansour Eman
El-Badry Yaser A.
El-Tokhy Afaf
Ayyad Rezed
Abd-Rabou Ahmed A.
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Abstract
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An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, 1H NMR, 13C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.
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KEYWORD
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Diazepines, Pyrimidines, Anticonvulsant activity, Antiproliferative activity
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