Table 1.

Antiviral and cytotoxicity data of 13-38 and 40^*

Compound	R1	R2	R3	R4	HIV-1 IIIB in H9 cells
					EC50a (μM)	CC50b (μM)	SIc
13	OMe	NO2	H	NO2	3.840	>61.12	>16
14	OMe	NO2	Me	NO2	2.990	>59.10	>20
15	OMe	NO2	Br	NO2	3.630	51.23	14
16	Me	NO2	Br	NO2	4.310	52.97	12
17	Cl	NO2	Br	NO2	NA	—	—
18	NO2	NO2	Br	NO2	>49.7	>49.70	>1
19	CN	NO2	Br	NO2	0.172	>51.76	>301
20	CN	NO2	H	NO2	0.545	>61.88	>113
21	CN	NO2	CN	NO2	4.190	>58.28	>14
22	CN	NO2	Me	NO2	0.280	>59.81	>214
23	CN	NO2	CHO	NO2	1.530	57.87	38
24	CN	H	Br	NO2	0.317	>57.08	>180
25	CN	H	H	NO2	3.147	69.64	22
26	CN	H	CN	NO2	0.208	>65.10	>313
27	CN	H	Me	NO2	0.067	>67.02	>1,000
28	CN	H	CHO	NO2	2.190	14.20	6
29	CN	H	Br	NH2	0.047	44.61	949
30	CN	H	CN	NH2	0.070	49.77	711
31	CN	H	Me	NH2	0.073	51.02	699
32	CN	NH2	Br	NH2	0.161	38.38	238
33	CN	NH2	H	NH2	3.226	53.20	16
34	CN	NH2	CN	NH2	0.030	50.95	1,698
35	CN	NH2	Me	NH2	0.070	50.00	714
36	CN	NO2	Br	NH2	0.016	45.47	2,842
37	CN	NO2	CN	NH2	0.003	62.66	20,887
38	CN	NO2	Me	NH2	0.062d	32.22d	520
40	Hydrochloride salt of 36				0.012	36.42	3,035
AZT					0.052	1873	36,019

^*Assays using H9 cells were performed at Panacos Pharmaceuticals, Inc., Gaithersburg, Maryland, USA. Results are averages of three independent assays. Standard deviations were not provided by Panacos.

^aConcentration of a compound that causes 50% inhibition of HIV-1 IIIB replication.

^bConcentration of a compound that causes cytotoxicity to 50% cells.

^cSI (selective index) = CC₅₀/EC_50.

^dData from Duke University, USA. NA: not active.