Anti-HIV-1 Activity of Indolyl Glyoxamides
Medicinal Chemistry, 2012, Vol. 8, No. 5 833
Table 1. Anti-HIV-1 Activity of Indolyl Glyoxamide Derivatives (3a-i) in Vitro a
Compound
CC50 b) (μg/mL)
EC50c) (μg/mL)
TId)
3a
3b
3c
3d
3e
3f
96.05
>154.56
>200
18.67
22.76
47.12
9.50
5.16
>6.79
>4.28
>19.98
>27.15
7.97
>189.87
>185.46
9.58
6.83
1.50
3g
3h
3i
3.14
3.31
0.97
98.18
4.35
49.45
26.07
10.94
0.00335
2.41
AZTe
1730.28
516,501.49
aValues are means of two separate experiments.
bCC50 (50% cytotoxic concentration), concentration of drug that causes 50% reduction in total C8166 cell number.
cEC50 (50% effective concentration), concentration of drug that reduces syncytia formation by 50%.
dTherapeutic Index (TI) is a ratio of the CC50 value/EC50 value.
eAZT was used as a positive control.
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and 4.35 μg/mL, and TI values of >27.15 and 49.45, respec-
tively. It demonstrated that introduction of the substituent R3
as the halogen atom and the position of R3 were generally
important to their activity.
CONFLICT OF INTEREST
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The author(s) confirm that this article content has no con-
flicts of interest.
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ACKNOWLEDGEMENTS
This work was financially supported in part by grants
from New Century Excellent University Talents, State Edu-
cation Ministry of China (NCET-06-0868), and the Key Pro-
ject of Chinese Ministry of Education (No. 107105). We also
would like to acknowledge the National Basic Research Pro-
gram of China (2009CB522306), the Eleventh Five-Year
Key Scientific and Technological Program of China
(2009ZX09501-029, 2008ZX10005-005), and Scientific and
Technological Projects of Yunnan (2007BC006).
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Received: August 12, 2011
Revised: April 16, 2012
Accepted: April 16, 2012