New Chalcones Containing 5-Fluorouracil Exhibiting in vitro Anti-Cancer Activity

Author(s): Luu Van Chinh , Truong Ngoc Hung , Nguyen Thi Nga , Le phong , Le Huu Cuong , Vu Tien Chinh , Soo Un Kim , Tran Khac Vu .

Journal Name: Letters in Organic Chemistry

Volume 12 , Issue 4 , 2015

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Graphical Abstract:


The synthesis and cytotoxicity evaluation of fourteen new chalcones containing 5-fluorouracil were introduced in which nine chalcones as Mannich bases 8a-i were synthesized from 2'-hydroxyacetophenone (1) in three steps including chloromethylation, N-alkylation and Claisen-Schmidt reactions. Other chalcones 14a-e were obtained from Click reaction between 1,3-dipropargyl-5-fluorouracil and azide derivatives of 2',4'-dihydroxychalcone. The bio-assay results showed that 11 chalcones (excluding 8d, 8f and 8h) exhibited cytotoxicity against four human cancer cell lines including Hep-G2, RD, LU-1 and FL in which compound 14e exhibited the most potent cytotoxicity against Hep-G2, RD, LU-1 and FL with IC50 values of 1.48, 10.59, 3.64 and 7.02 μg/mL, respectively.

Keywords: Chalcone, 5-fluorouracil, N-alkylation, click reaction and cytotoxicity.

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Article Details

Year: 2015
Page: [251 - 261]
Pages: 11
DOI: 10.2174/1570178612666150226230109
Price: $58

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