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Anti‐Tumor Activity of New Artemisinin–Chalcone Hybrids
Author(s) -
Xie Lijun,
Zhai Xin,
Liu Chun,
Li Peng,
Li Yangxiong,
Guo Guoxian,
Gong Ping
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000391
Subject(s) - chalcone , hela , dihydroartemisinin , moiety , chemistry , artemisinin , selectivity , stereochemistry , cell culture , in vitro , combinatorial chemistry , biochemistry , biology , catalysis , immunology , plasmodium falciparum , genetics , malaria
In an attempt to develop potent and selective anti‐tumor agents, three new series of artemisinin–chalcone hybrids 10a – 10g , 11a – 11g and 12a–12h were designed, synthesized and screened for their anti‐tumor activity against five cell lines (HT‐29, A549, MDA‐MB‐231, HeLa and H460) in vitro . Among compounds 10a–g and 11a–11g , most of them displayed enhanced activity and good selectivity toward HT‐29 and HeLa cell lines with IC 50 values ranging from 0.12 to 0.85 µM as compared with DHA (dihydroartemisinin). Compounds 10a and 11a are most active toward HeLa cells with IC 50 values of 0.12 and 0.19 µM. The results revealed that the presence of chalcone moiety is beneficial to their activity and selectivity. In addition, compounds 12a ‐ 12h containing a ‘reversed chalcone’ moiety showed only slight improvement in activity than those of DHA.