A series of artemisinin-indoloquinoline hybrids were designed and synthesized in an attempt to develop potent and selective anti-tumor agents. Compounds
7a–
7f,
8 and
9 were prepared and characterized. Their antiproliferative activities against MV4-11, HCT-116, A549, and BALB/3T3 cell lines
in
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A series of artemisinin-indoloquinoline hybrids were designed and synthesized in an attempt to develop potent and selective anti-tumor agents. Compounds
7a–
7f,
8 and
9 were prepared and characterized. Their antiproliferative activities against MV4-11, HCT-116, A549, and BALB/3T3 cell lines
in vitro were tested. Nearly all of the tested compounds (
7–
9, except for compounds
7d and
7e against HCT-116) showed an increased antitumor activity against HCT-116 and A549 cell lines when compared to the dihydroartemisinin control. Especially for the artemisinin-indoloquinoline hybrid
8, with an 11-aminopropylamino-10
H-indolo[3,2-
b]quinoline substituent, the antiproliferative activity against the A549 cell line had improved more than ten times. The IC
50 value of hybrid
8 against A549 cell lines was decreased to 1.328 ± 0.586 μM, while dihydroartemisin showed IC
50 value of >20 µM in the same cell line. Thus, these results have proven that the strategy of introducing a planar basic fused aromatic moiety, such as the indoloquinoline skeleton, could improve the antiproliferative activity and selectivity towards cancer cell lines.
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