. Author manuscript; available in PMC: 2008 Aug 12.

Published in final edited form as: J Med Chem. 2006 Sep 7;49(18):5462–5469. doi: 10.1021/jm0601912

Table 2.

Comparison of Anti-HIV Activities of Selected Derivatives Against Several HIV-1 Strains in MT-4 Cells

compound	EC₅₀ (μM) in different viral strains			IC₅₀ (μM)
compound	NL4−3	PI-R	FHR-2	IC₅₀ (μM)
8	0.096	0.43	NS	>5^*
10	0.010	0.006	0.05	12.2
19	0.045	0.088	2.78	23.5
20	0.0085	0.021	0.13	21.0
AZT	0.013	0.019	0.019	>37.5

NL4−3 is a T-cell adapted HIV-1 strain, X4 wild type virus; PI-R is an HIV-1 strain, HIV-1 M46I/L63P/V82T/I84V, resistant to multiple protease inhibitors;¹⁷ and FHR-2 is an HIV-1 strain resistant to 8.⁷ EC₅₀ is the concentration that inhibits HIV-1 replication by 50%; and IC₅₀ is the concentration that decreases 50% of viable cell number.

The highest concentration tested for DSB was 5 μM; there was no observable cytotoxicity at this concentration. NS: No suppression at testing concentration, 5 μM.