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. Author manuscript; available in PMC: 2013 Dec 17.
Published in final edited form as: Bioorg Med Chem. 2011 Mar 1;19(6):10.1016/j.bmc.2011.01.047. doi: 10.1016/j.bmc.2011.01.047

Table 2.

Structure and HIV-1 integrase inhibitory activities of synthesized compounds

graphic file with name nihms272252u3.jpg
Comp. Ar R2 R1 X Activity (IC50μM)
3′-Pa STb
8 4-F-Ph NH Br CHO >100 8 ± 1
60 2,5-di-Cl-Ph CH2 F COOH >100 57 ± 5
61 4-F-Ph NH Br COOH >100 15 ± 3
62 4-F-Ph NH H CH3 >100 >100
63 4-F-Ph NH Br H >100 >100
S1360c N/A N/A N/A N/A 11 ± 2 0.6 ± 0.1
a

3-P = 3′-processing,

b

ST = strand transfer,

c

S1360 = standard