Table 2.

Antiviral activity of the target compounds against HIV-1 mutant strains.

Compd.	EC50 (μmol/L)a
	L100I	K103N	Y181C	Y188L	E138K	F227L + V106A	RES056
R1L2	0.68 ± 0.39	0.41 ± 0.11	0.61 ± 0.13	6.42 ± 1.40	0.86 ± 0.36	1.75 ± 0.20	3.38 ± 0.89
R1L3	0.54 ± 0.42	0.73 ± 0.14	1.19 ± 0.3	7.14 ± 1.4	0.21 ± 0.14	1.26 ± 0.38	5.97 ± 0.65
R1L4	0.16 ± 0.085	0.31 ± 0.068	0.31 ± 0.068	1.52 ± 0.27	0.13 ± 0.085	0.31 ± 0.034	>103.03
R1L5	0.17 ± 0.017	0.63 ± 0.017	0.23 ± 0.017	2.53 ± 0.18	0.18 ± 0.017	0.38 ± 0.13	>113.2
R2L2	0.66 ± 0.23	0.9 ± 0.38	0.85 ± 0.035	>105.8	1.11 ± 0.17	1.58 ± 0.45	>105.8
R2L3	0.32 ± 0.00	0.66 ± 0.085	0.83 ± 0.068	5.98 ± 0.31	0.25 ± 0.00	0.97 ± 0.051	>162.9
R2L4	0.18 ± 0.00	0.33 ± 0.033	0.33 ± 0.00	0.80 ± 0.083	0.25 ± 0.05	0.28 ± 0.033	>22.48
R2L5	0.094 ± 0.047	0.57 ± 0.00	0.19 ± 0.016	1.28 ± 0.44	0.13 ± 0.049	0.28 ± 0.065	>109.8
R3L2	0.95 ± 0.085	0.59 ± 0.10	1.00 ± 0.17	>211.84	1.15 ± 0.00	6.17 ± 1.14	>211.84
R3L3	0.35 ± 0.017	0.73 ± 0.12	1.03 ± 0.050	3.29 ± 0.066	0.31 ± 0.050	1.77 ± 0.033	4.92 ± 1.27
R3L4	0.13 ± 0.018	0.50 ± 0.16	0.40 ± 0.11	0.87 ± 0.065	0.23 ± 0.032	0.36 ± 0.032	1.88 ± 0.68
R3L5	0.13 ± 0.0063	0.9 ± 0.079	0.30 ± 0.00	2.47 ± 0.16	0.25 ± 0.032	0.54 ± 0.14	25.14 ± 0.047
R4L2	0.21 ± 0.036	0.36 ± 0.16	0.37 ± 0.14	3.00 ± 0.053	0.37 ± 0.11	0.83 ± 0.12	3.23 ± 0.018
R4L3	0.24 ± 0.035	0.45 ± 0.10	0.69 ± 0.017	2.84 ± 0.052	0.26 ± 0.017	1.04 ± 0.035	3.55 ± 0.35
R4L4	0.056 ± 0.036	0.19 ± 0.051	0.20 ± 0.034	1.27 ± 0.20	0.063 ± 0.003	0.29 ± 0.12	>211.47
R4L5	0.074 ± 0.010	0.51 ± 0.21	0.18 ± 0.017	1.67 ± 0.35	0.073 ± 0.02	0.38 ± 0.017	>31.17
R5L2	0.77 ± 0.035	0.84 ± 0.035	0.89 ± 0.018	3.07 ± 0.12	1.26 ± 0.00	1.75 ± 0.053	3.37 ± 0.21
R5L3	0.33 ± 0.034	0.92 ± 0.41	0.98 ± 0.051	3.34 ± 0.017	0.27 ± 0.017	1.22 ± 0.051	4.09 ± 0.00
R5L4	0.025 ± 0.002	0.067 ± 0.005	0.054 ± 0.002	0.15 ± 0.010	0.032 ± 0.018	0.082 ± 0.035	>4.58
R5L5	0.077 ± 0.023	0.56 ± 0.13	0.21 ± 0.00	1.70 ± 0.52	0.16 ± 0.016	0.34 ± 0.082	11.88 ± 4.90
R6L2	0.75 ± 0.064	0.95 ± 0.16	1.01 ± 0.032	≥33.74	1.27 ± 0.11	2.73 ± 0.48	≥12.17
R6L3	0.78 ± 0.14	1.04 ± 0.19	1.32 ± 0.19	5.26 ± 1.04	0.47 ± 0.20	1.48 ± 0.11	>88.08
R6L4	0.32 ± 0.15	0.69 ± 0.11	0.60 ± 0.031	1.00 ± 0.15	0.78 ± 0.54	0.51 ± 0.092	>26.91
R6L5	0.12 ± 0.039	0.74 ± 0.090	0.35 ± 0.00	2.47 ± 0.030	0.32 ± 0.015	0.68 ± 0.075	>37.86
R7L2	0.17 ± 0.041	0.22 ± 0.00	0.31 ± 0.16	2.66 ± 0.17	0.36 ± 0.017	1.04 ± 0.35	3.09 ± 0.50
R7L3	0.098 ± 0.052	0.22 ± 0.00	0.57 ± 0.25	0.19 ± 0.19	0.61 ± 0.12	2.61 ± 0.12	9.00 ± 0.51
R7L4	0.074 ± 0.021	0.13 ± 0.048	0.18 ± 0.016	1.53 ± 0.72	0.051 ± 0.018	0.26 ± 0.00	>89.33
R7L5	0.061 ± 0.0032	0.43 ± 0.14	0.19 ± 0.00	3.14 ± 0.95	0.052 ± 0.009	0.37 ± 0.11	>114.72
R8L2	0.80 ± 0.094	1.18 ± 0.091	1.00 ± 0.091	6.24 ± 0.65	1.20 ± 0.018	1.81 ± 0.18	4.63 ± 1.54
R8L3	0.50 ± 0.14	1.03 ± 0.19	1.06 ± 0.018	3.54 ± 0.34	0.28 ± 0.018	1.65 ± 0.27	5.38 ± 1.29
R8L4	0.13 ± 0.059	0.47 ± 0.069	0.54 ± 0.00	1.05 ± 0.035	0.19 ± 0.017	0.36 ± 0.035	>86.52
R8L5	0.17 ± 0.017	1.23 ± 0.22	0.73 ± 0.34	2.71 ± 0.13	0.20 ± 0.051	1.26 ± 0.34	>43.31
R9L2	0.26 ± 0.11	0.24 ± 0.037	0.26 ± 0.073	2.81 ± 0.29	0.22 ± 0.073	1.12 ± 0.35	3.14 ± 0.11
R9L3	0.18 ± 0.054	0.32 ± 0.072	0.70 ± 0.27	3.08 ± 0.25	0.055 ± 0.018	0.80 ± 0.25	4.76 ± 0.80
R9L4	0.028 ± 0.0087	0.15 ± 0.045	0.15 ± 0.033	0.87 ± 0.17	0.031 ± 0.007	0.28 ± 0.052	>114.95
R9L5	0.044 ± 0.005	0.34 ± 0.051	0.22 ± 0.017	1.46 ± 0.56	0.036 ± 0.007	0.22 ± 0.085	>119.33
R10L2	0.14 ± 0.046	0.29 ± 0.055	0.29 ± 0.018	2.20 ± 0.40	0.12 ± 0.033	1.48 ± 0.27	4.60 ± 0.31
R10L3	0.10 ± 0.032	0.20 ± 0.036	0.20 ± 0.018	2.32 ± 0.11	0.043 ± 0.005	0.54 ± 0.27	7.77 ± 2.32
R10L4	0.017 ± 0.002	0.068 ± 0.012	0.045 ± 0.010	0.54 ± 0.087	0.017 ± 0.007	0.087 ± 0.035	5.26
R10L5	0.046 ± 0.014	0.19 ± 0.034	0.11 ± 0.022	0.73 ± 0.034	0.029 ± 0.012	0.14 ± 0.075	10.61 ± 6.70
R11L2	0.25 ± 0.071	0.21 ± 0.053	0.28 ± 0.036	2.68 ± 0.25	0.20 ± 0.036	1.23 ± 0.43	3.04 ± 0.21
R11L3	0.16 ± 0.078	0.28 ± 0.035	0.61 ± 0.14	7.12 ± 0.76	0.068 ± 0.002	0.88 ± 0.52	12.84 ± 10.12
R11L4	0.063 ± 0.025	0.17 ± 0.017	0.20 ± 0.017	1.74 ± 0.32	0.036 ± 0.005	0.29 ± 0.034	>189.54
R12L2	0.46 ± 0.18	0.50 ± 0.089	0.55 ± 0.089	3.30 ± 0.30	0.44 ± 0.11	2.26 ± 0.55	4.94 ± 1.24
R12L3	0.26 ± 0.087	0.45 ± 0.12	0.75 ± 0.21	3.38 ± 0.45	0.11 ± 0.043	0.99 ± 0.14	4.73 ± 1.04
R12L4	0.063 ± 0.017	0.24 ± 0.068	0.19 ± 0.034	1.45 ± 0.41	0.049 ± 0.012	0.24 ± 0.034	>173.28
R13L2	0.053 ± 0.022	0.11 ± 0.020	0.18 ± 0.057	1.65 ± 0.39	0.055 ± 0.016	0.51 ± 0.12	32.57 ± 7.96
R14L2	0.95 ± 0.097	1.19 ± 0.26	1.42 ± 0.37	>31.20	0.74 ± 0.097	2.99 ± 0.68	>82.35
NVP	1.26 ± 0.60	5.33 ± 1.07	>9.52	>9.52	0.095 ± 0.031	>9.52	>9.52
EFV	0.032 ± 0.006	0.10 ± 0.019	0.007 ± 0.002	0.27 ± 0.016	0.007 ± 0.001	0.27 ± 0.048	0.48 ± 0.19
ETR	0.032 ± 0.028	0.015 ± 0.012	0.058 ± 0.041	0.083 ± 0.053	0.037 ± 0.030	0.088 ± 0.076	0.15 ± 0.12
IAS-4	0.047 ± 0.021	0.056 ± 0.005	0.25 ± 0.018	0.56 ± 0.14	0.04 ± 0.02	0.23 ± 0.070	7.45 ± 2.25
IAS-0	0.015 ± 0.0086	0.017 ± 0.0060	0.039 ± 0.0028	1.1 ± 0.63	0.90 ± 0.065	0.047 ± 0.023	1.8 ± 0.29

^aEC₅₀: Concentration of compound that decreases 50% HIV-1-induced cytopathy of MT-4 cells.