New Chalcones Containing Nucleosides Exhibiting In Vitro Anti-cancer Activities
Luu Van Chinh,
Truong Ngoc Hung,
Nguyen Thi Nga,
Le Mai Huong,
Tran Thi Hong Ha,
Soo Un Kim,
Tran Khac Vu.
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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