New Chalcones Containing Nucleosides Exhibiting In Vitro Anti-cancer Activities

Author(s): Luu Van Chinh, Truong Ngoc Hung, Nguyen Thi Nga, Le phong, Le Mai Huong, Tran Thi Hong Ha, Soo Un Kim, Tran Khac Vu.

Journal Name: Letters in Organic Chemistry

Volume 11 , Issue 7 , 2014

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Graphical Abstract:


Twenty-one new chalcones 9a-m (excluding 9e, 9j and 9l) and 10a-m (excluding 10j and 10l), containing nucleobases were synthesized from 2'-hydroxyacetophenone (1) by the reactions including chloromethylation, nucleophilic substitution with thymine and uracil, and Claisen-Schmidt reactions. These new chalcones were evaluated for in vitro cytotoxicity against five human cancer cell lines: SK-LU-1, Hep-G2, MCF7, SW480 and P388. The results showed that most of the tested chalcones exhibited inhibitory activity against five cancer cell lines except 10h, and 10i. Among the synthesized chalcones, compound 10c exhibited most potent cytotoxicity against MCF-7, SK-LU-1, SW480, HepG2 and P388 with IC50 values of 4.42, 4.81, 5.27, 3.67 and 4.11μg/mL, respectively.

Keywords: Chalcones, Claisen-Schmidt, cytotoxicity, 2'-hydroxyacetophenone, thymine, uracil.

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Article Details

Year: 2014
Page: [534 - 545]
Pages: 12
DOI: 10.2174/1570178611666140401221121
Price: $58

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