Table 1.

Anti-HIV-1 (IIIB) and HIV-2 (ROD) activity, cytotoxicity and SI of target compounds 11–32.

Compd.	R1	R2	EC50 (nmol/L)a		CC50 (μmol/L)b	SIc
			IIIB	ROD		IIIB	ROD
11		SO2NH2	17.7 ± 4.83	4148 ± 1785	13.5 ± 3.94	762	3
12		CONH2	93.3 ± 82.8	25,289 ± 18,400	28.9 ± 15.6	310	1
13		SO2NH2	63.6 ± 11.4	6805 ± 1225	15.6 ± 4.97	246	2
14		CONH2	57.5 ± 12.7	3181 ± 832	15.8 ± 7.04	275	5
15		SO2NH2	49.5 ± 14.8	5111 ± 1707	21.5 ± 0.89	435	4
16		CONH2	203 ± 51.5	>20,535	≥20.5	≥101	NAd
17		SO2NH2	31.6 ± 17.7	4802 ± 916	15.4 ± 5.86	489	3
18		CONH2	240 ± 94.3	>17,044	17.0 ± 12.9	71	<1
19		SO2NH2	43.8 ± 15.6	6135 ± 272	21.3 ± 1.26	487	3
20		CONH2	47.7 ± 11.8	3842 ± 1765	17.5 ± 6.18	367	5
21		SO2NH2	61.1 ± 10.3	>16,635	16.6 ± 4.65	272	<1
22		CONH2	52.6 ± 11.4	5035 ± 685	13.4 ± 5.94	256	3
23		SO2NH2	11.3 ± 2.07	3283 ± 1255	16.9 ± 4.77	1492	5
24		CONH2	12.8 ± 2.73	≥5655	6.80 ± 3.13	532	<1
25		SO2NH2	17.0 ± 5.78	5560 ± 42.3	5.31 ± 2.56	312	1
26		CONH2	9.93 ± 1.27	>5488	5.48 ± 2.12	552	<1
27		SO2NH2	13.3 ± 2.60	4916 ± 2247	14.0 ± 8.28	1054	3
28		CONH2	23.4 ± 16.9	>4169	4.16 ± 1.75	178	<1
29		SO2NH2	79.2 ± 48.7	>18,381	18.3 ± 4.50	232	<1
30		CONH2	176 ± 26.4	>23,535	23.5 ± 0.38	134	<1
31		SO2NH2	882 ± 323	>110,175	110 ± 1.46	125	<1
32		CONH2	163 ± 57.8	4659 ± 824	19.8 ± 4.47	121	4
NVP	–	–	186 ± 59.0	>9510	>9.51	>51	NAd
EFV	–	–	5.25 ± 1.98	>5330	>6.33	>1205	NAd
ETR	–	–	5.03 ± 1.68	>4594	>4.59	>913	NAd
K-5a2e	–	–	1.4 ± 0.4	≥227,890	≥227	>159,101	NAd

^aEC₅₀: concentration of compound required to achieve 50% protection of MT-4 cell cultures against HIV-1-induced cytotoxicity, as determined by the MTT method. A smaller EC₅₀ values means that the compound has greater activity.

^bCC₅₀: concentration required to reduce the viability of mock-infected cell cultures by 50%, as determined by the MTT method. A larger CC₅₀ values means that the compound has lower toxicity.

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

^dNA: stands for≥1 or<1.

^eData were reported in ref. 14. –Not applicable.