Table 3.

Anti-HIV activity, cytotoxicity and SI values of target compounds 22-30.

Compds	R1	R2	EC50(nM)a		CC50 (μM)b	SIc
			IIIB	RES056		IIIB	RES056
22a		SO2NH2	4.60±1.14	22.9±7.07	9.25±5.17	2011	404
22b		SO2CH3	5.74±1.38	26.3±6.99	7.20±5.41	1255	273
22c		CONH2	4.19±0.45	23.3±7.67	10.2±6.69	2428	436
23a		SO2NH2	5.75±1.27	34.3±13.2	5.50±1.98	957	160
23b		SO2CH3	3.95±0.54	30.0±12.4	2.10±0.95	533	70
23c		CONH2	7.28±1.27	40.3±10.7	6.27±1.21	861	156
24a		SO2NH2	4.16±0.98	23.0±5.85	4.37±1.15	1105	190
24b		SO2CH3	4.55±0.61	31.5±5.50	5.34±2.87	1174	169
24c		CONH2	3.53±0.38	18.1±0.30	6.51±2.82	1845	358
25a		SO2NH2	6.37±1.27	38.8±12.6	8.46±2.08	1326	218
25b		SO2CH3	4.75±1.19	25.1±7.23	5.03±1.72	1057	200
25c		CONH2	8.26±1.79	53.4±30.9	15.5±5.32	1878	290
26a		SO2NH2	4.30±0.54	20.9±4.14	3.89±1.01	904	185
26b		SO2CH3	4.23±1.06	33.3±7.24	2.04±0.88	482	61
26c		CONH2	4.14±0.43	81.7±61.7	19.1±1.66	4627	243
27a		SO2NH2	4.42±0.52	26.9±12.1	6.60±2.69	1493	246
27b		SO2CH3	4.52±0.55	33.2±9.31	3.21±0.61	711	97
27c		CONH2	7.00±4.69	32.2±8.02	9.45±4.34	1351	293
28a		SO2NH2	5.04±2.07	25.8±9.45	20.4±4.11	4063	793
28b		SO2CH3	4.57±1.24	22.4±1.87	23.5±0.96	5151	1049
28c		CONH2	4.78±2.57	23.1±3.80	25.3±1.84	5297	1092
29a		SO2NH2	5.80±1.37	33.5±6.89	2.91±0.65	503	87
29b		SO2CH3	5.29±2.14	26.2±4.80	2.36±0.93	447	90
29c		CONH2	6.56±2.11	30.2±6.55	12.8±3.73	1956	424
30a		SO2NH2	5.80±1.53	28.2±6.82	17.1±4.82	2956	607
30b		SO2CH3	6.04±1.76	25.5±2.89	6.05±1.18	1003	237
30c		CONH2	4.56±1.49	20.4±0.98	20.9±3.65	4586	1021
ETR	-	-	3.53±0.70	52.2±24.2	>4.59	>1300	>88
RPV			1.0±0.27	10.7±7.96	3.98	3989	371

^aEC₅₀: concentration of compound required to achieve 50% protection of MT-4 cell cultures against HIV-1-induced cytopathicity, as determined by the MTT method.

^bCC₅₀: concentration required to reduce the viability of mock-infected cell cultures by 50%, as determined by the MTT method.

^cSI: selectivity index, the ratio of CC₅₀/EC₅₀.