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. Author manuscript; available in PMC: 2009 May 6.
Published in final edited form as: J Am Chem Soc. 2008 Jun 28;130(29):9492–9499. doi: 10.1021/ja8019214

Table 7.

Benzylic Analogues: Anti-HIV-1 Activity (EC50) and Cytotoxicity (CC50)

graphic file with name nihms88205t6.jpg
compd R R′ X Y EC50a(µM) CC50a(µM)
8 Cl Cl CH2 NH 0.82 20
15 Cl Cl NH NH > 100 > 100
16 Cl Cl CH2 CH2 18 43
13 Cl CN CH2 NH 0.13 40
17 Cl CN NH NH 9.8 > 100
18 Cl CN NCH3 NH 0.27 > 100
19b Cl CN CHCH3 NH 1.20 54
20b F CN CHCH3 NH 0.13 8.5
a

See footnotes in Table 4.

b

Racemate.