. Author manuscript; available in PMC: 2010 Sep 15.

Published in final edited form as: Bioorg Med Chem Lett. 2009 Jul 19;19(18):5482–5485. doi: 10.1016/j.bmcl.2009.07.080

Table 1.

Inhibitory activity of 4a-4g and 5a-5g on HIV-1_IIIB replication in MT-2 cells^a

Compds	R	CC₅₀ (μM)^b	EC₅₀ (μM)^c	SI^d
4a	H	110.2±0.0	1.028±0.139	107
4b	CH₃	503.2±5.2	0.118±0.053	4,264
4c	CH₂OH	115.8±14.1	0.192±0.005	603
4d	I	148.5±31.2	2.428±0.309	61
4e	CN	50.13±2.60	0.135±0.286	371
4f	C≡CC(OH)Me₂	8.91±0.0	23.28±10.48	<1
4g	C≡CH	173.6±46.0	0.677±0.286	256
5a	H	29.9±2.3	0.576±0.182	52
5b	CH₃	10.55±0.41	0.058±0.026	182
5c	CH₂OH	2.19±0.41	0.006±0.002	391
5d	I	23.49±5.77	0.079±0.007	297
5e	CN	31.78±10.37	0.0014±0.0023	22,700
5f	C≡CC(OH)Me₂	3.54±1.07	1.578±0.097	2
5g	C≡CH	8.25±0.51	0.424±0.282	20

Compounds were tested in triplicate and the data are presented as means ± SD.

XTT assay was used to determine the 50% cytotoxic concentration (CC₅₀).

ELISA was used to determine p24 production, based on which the 50% effective concentration (EC₅₀) for inhibiting HIV-1 replication was calculated.

Selectivity index (SI) = CC₅₀/ EC₅₀