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D.-Q. Song et al. / Bioorg. Med. Chem. Lett. 19 (2009) 755–758
Table 3
Activities of 16c and 16g in human hepatoma cell linesa
b
Cell line
Human tumor
IC50 (lM)
16c
16g
1
VCR
Bel-7402
HepG2
SMMC-7721
Hepatoma
Hepatoma
Hepatoma
1.40 0.10
0.82 0.28
0.67 0.28
1.20 0.16
0.90 0.36
0.93 0.29
1.12 0.1
1.20 0.20
9.26 0.21
0.04 0.01
ND
52.21 9.67
ND, not done.
a
Antiproliferative activity was done with MTT assay.
IC50, a drug concentration required to inhibit human tumor cells proliferation by 50% after 72 h treatment.
b
Figure 3. Cell cycle analysis. CEM cells were untreated or treated with 1 (3.2 lM), or VCR (0.1 lM), or 16c (0.69 lM), respectively, for 12 h at 37 °C. Cells were collected and
fixed with methanol followed by DNA fluorescent staining. Flow cytometric cell cycle analysis was done with a conventional cell cycle test protocol.
Acknowledgment
This study was supported by the National Natural Science Foun-
dation of the PR China (Grant 30371673).
Supplementary data
Supplementary data associated with this article can be found, in
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Figure 4. Morphological examination. CEM cells were treated with compound 1
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l
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a
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the p–
p conjugation between the aromatic ring and formylurea
group is an essential element for the high cancericidal activity.
Also, suitable aryl substitutions at the N0-end not only enhance
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