Table 1.

Anti-HIV activity and cytotoxicity of 5′-O-aliphatic and amino acid esters of (−)-β-d-(2R,4R)-dioxolane-thymine (DOT).

Compounds	HIV-1LAI (μM)a		Cytotoxicity (IC50, μM)b
	EC50	EC90	PBM	CEM	Vero
1	2.9	12.3	>100	99.4	>100
2	0.4	2.5	>100	>100	49.0
3	0.6	4.3	>100	>100	>100
4	0.4	3.2	>100	>100	>100
5	23.5	>100	>100	>100	92.2
6	1.3	14.5	>100	>100	18.1
7	4.7	15.1	>100	>100	>100
8	1.3	3.9	>100	>100	>100
9	1.4	9.7	>100	>100	>100
10	1.5	10.2	>100	>100	>100
11	2.5	8.4	>100	>100	>100
12	2.2	7.6	>100	>100	>100
13	0.98	8.3	>100	>100	>100
14	0.88	4.4	>100	>100	>100
15	1.0	5.2	>100	>100	>100
16	0.56	4.9	>100	>100	>100
17	0.98	6.5	>100	>100	>100
18	3.3	12.4	>100	>100	>100
19	3.0	9.9	>100	>100	>100
20	0.89	6.3	>100	>100	>100
21	1.4	7.3	>100	>100	>100
22	1.7	8.0	>100	>100	>100
DOT	0.68	4.0	>100	>100	>100
AZT	0.007	0.04	>100	14.3	50.6

^aAnti-HIV activity against HIV-1_LAI in PBM cells.

^bAssay in PBM, CEM and Vero cells.