Table 2.

Anti-HIV-1 Activity (EC₅₀) and cytotoxicity (CC₅₀), μM^a

Compound	R	X	WT	EC50		CC50
				Y181C	K103N/Y181C
1a	H	H	0.013	NA	NA	8
1b	H	Cl	0.0062	0.420	NA	10
1c	F	Cl	0.0091	0.910	NA	7
1d	Me	Cl	0.011	0.210	7.2	31
1e	Et	Cl	0.0013	0.0069	0.21	10
1f	i-Pr	Cl	0.0052	0.0072	0.12	5
1g	c-Pr	Cl	0.024	1.5	10.7	65
1h	CH2c-Pr	Cl	0.068	1.2	15.0	29
1ib	s-Bu	Cl	0.120	0.15	2.8	40
1j	OEt	Cl	0.028	0.048	0.75	15
1k	CH2OMe	Cl	0.0036	0.690	6.3	15
2a	H		0.031	3.2	4.5	16
2b	Et		0.005	0.060	0.80	5
3c	t-Bu	Cl	1.3	NA	NA	6
nevirapine			0.11	NA	NA	>100
efavirenz			0.002	0.010	0.030	15
etravirine			0.001	0.008	0.005	11
rilpivirine			0.00067	0.00065	0.002	8

^aResults using human MT-2 cells. Antiviral and toxicity curves used triplicate samples at each concentration.

NA = not active.

^bRacemic.

^cThe 4-t-butyl-2,6-dichlorobenzyl analog of 1b.