Table 1.

Anti-HIV activities of 9a–9e in cellular assay and aqueous solubility^a

	R1	EC50 (nM)b	CC50 (μM)c	SId	Aqueous Solubility (μg/mL)
					pH 7.4	pH 2.0
9a	COOCH3	2.74 ± 0.71	>22.8	>8465	1.30	1.75
9b	COOH	230 ± 38	14.9	65	117	4.40
9c	CONH2	0.87 ± 0.28	>23.6	>27126	0.63	2.10
9d	CONHCH3	5.72 ± 0.94	>9.2	>1606	1.32	8.63
9e	CH2OH	0.53 ± 0.13	16.3	30754	3.23	21.0
3e	NO2	0.38 ± 0.07	>47.1	>123947	0.29	0.29
2 (TMC278)		0.52 ± 0.14	19.4	37305	0.24	156

^aHIV-1 NL3-4 (wild-type) virus in TZM-bl cell lines.

^bConcentration of compound that causes 50% inhibition of viral replication and presented as mean ± standard deviation (SD) in at least triplicate.

^cConcentration of compound that causes cytotoxicity to 50% of cells.

^dSelectivity index (SI) is the ratio of CC₅₀/EC₅₀.

^eCompound and activity data were published previously¹²