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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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 and Tran Khac Vu

Volume 12 , Issue 4 , 2015

Page: [251 - 261] Pages: 11

DOI: 10.2174/1570178612666150226230109

Price: $65


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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