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

作者：Luu Van Chinh^*; Truong Ngoc Hung; Nguyen Thi Nga; Le Phong; Le Huu Cuong; Vu Tien Chinh; Kim Soo Un; Tran Khac Vu

来源：Letters in Organic Chemistry, 2015, 12(4): 251-261.

DOI：10.2174/1570178612666150226230109

• Chalcone
• 5-fluorouracil
• N-alkylation
• click reaction
• cytotoxicity

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 mu g/mL, respectively.

• 出版日期2015
• 单位中国农业大学