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. Author manuscript; available in PMC: 2012 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2010 Nov 25;19(1):77–90. doi: 10.1016/j.bmc.2010.11.045

Table 1.

Antiviral activity of 1 and its analogs against HIV-1 IIIB in MT-2 cells.

graphic file with name nihms256229u1.jpg
No. R1 R2 R3 R4 R5 μM (± SD)
IC50 CC50
1 graphic file with name nihms256229t1.jpg graphic file with name nihms256229t2.jpg H H CH3 4.02 ± 0.28 >67.13
2 graphic file with name nihms256229t3.jpg graphic file with name nihms256229t4.jpg H H CH3 4.23 ± 0.39 >64.7
3 graphic file with name nihms256229t5.jpg graphic file with name nihms256229t6.jpg H H CH3 7.25 ± 0.54 >64
4 graphic file with name nihms256229t7.jpg graphic file with name nihms256229t8.jpg H H CH3 >16.5 >66.1
5 graphic file with name nihms256229t9.jpg graphic file with name nihms256229t10.jpg H H CH3 2.67 ± 0.5 9.2 ±1.0
6 graphic file with name nihms256229t11.jpg graphic file with name nihms256229t12.jpg CH3 H H 1.06 ± 0.05 >61.45
7 graphic file with name nihms256229t13.jpg graphic file with name nihms256229t14.jpg CH3 H H >16.7 ND
8 graphic file with name nihms256229t15.jpg graphic file with name nihms256229t16.jpg CH3 H H 2.16 ± 0.07 >55.4
9 graphic file with name nihms256229t17.jpg graphic file with name nihms256229t18.jpg CH3 H H 9.28 ± 0.68 >67.1
10 graphic file with name nihms256229t19.jpg CF3 CH3 H H >27.5 ND
11 graphic file with name nihms256229t20.jpg graphic file with name nihms256229t21.jpg CH3 H H >24.5 ND
12 graphic file with name nihms256229t22.jpg graphic file with name nihms256229t23.jpg CH3 H H >25.6 ND
13 graphic file with name nihms256229t24.jpg graphic file with name nihms256229t25.jpg CH3 H H 9.2 ± 0.7 70.7 ± 5.4
14 graphic file with name nihms256229t26.jpg graphic file with name nihms256229t27.jpg CH3 H H >23.6 ND
15 graphic file with name nihms256229t28.jpg graphic file with name nihms256229t29.jpg CH3 H H 7.1 ± 0.4 >20.4
16 graphic file with name nihms256229t30.jpg graphic file with name nihms256229t31.jpg CH3 H H >25.2 ND
17 graphic file with name nihms256229t32.jpg graphic file with name nihms256229t33.jpg CH3 H H 8.2 ± 1.2 >23.5
18 graphic file with name nihms256229t34.jpg graphic file with name nihms256229t35.jpg CH3 H H >21.9 ND
19 graphic file with name nihms256229t36.jpg graphic file with name nihms256229t37.jpg CH3 H H >24.8 ND
20 graphic file with name nihms256229t38.jpg graphic file with name nihms256229t39.jpg CH3 H H >24.1 ND
21 graphic file with name nihms256229t40.jpg graphic file with name nihms256229t41.jpg CH3 H H >23.6 ND
22 graphic file with name nihms256229t42.jpg graphic file with name nihms256229t43.jpg CH3 H H >26.6 ND
23 graphic file with name nihms256229t44.jpg graphic file with name nihms256229t45.jpg CH3 H H 4.7 ± 0.6 >24.5
24 graphic file with name nihms256229t46.jpg graphic file with name nihms256229t47.jpg CH3 H H >22.1 ND
25 graphic file with name nihms256229t48.jpg graphic file with name nihms256229t49.jpg CH3 H H >38.9 ND
26 graphic file with name nihms256229t50.jpg graphic file with name nihms256229t51.jpg CH3 H H 9.27 ± 0.3 44.5 ± 5.5
27 graphic file with name nihms256229t52.jpg graphic file with name nihms256229t53.jpg C2H5 H H >13.9 ND
28 graphic file with name nihms256229t54.jpg graphic file with name nihms256229t55.jpg C2H5 H H 12.3 ± 0.85 >127.4
29 graphic file with name nihms256229t56.jpg graphic file with name nihms256229t57.jpg OCH3 H H >13 ND
30 graphic file with name nihms256229t58.jpg graphic file with name nihms256229t59.jpg OCH3 H H 7.87 ± 1.0 >31
31 graphic file with name nihms256229t60.jpg graphic file with name nihms256229t61.jpg OCH3 H H >25.7 ND
32 graphic file with name nihms256229t62.jpg graphic file with name nihms256229t63.jpg CH3 H H 11.7 ± 1.2 >63.4
33 graphic file with name nihms256229t64.jpg graphic file with name nihms256229t65.jpg CH3 H H 11.8 ± 0.4 >64
34 graphic file with name nihms256229t66.jpg graphic file with name nihms256229t67.jpg CH3 H H >12.9 ND
35 graphic file with name nihms256229t68.jpg graphic file with name nihms256229t69.jpg CH3 H H 5.0 ± 0.2 12.7 ± 1.0
36 graphic file with name nihms256229t70.jpg graphic file with name nihms256229t71.jpg CH3 H CH3 8.6 ± 1.1 >96
37 graphic file with name nihms256229t72.jpg graphic file with name nihms256229t73.jpg OCH3 H H 7.9 ± 0.4 25 ± 1.0
38 graphic file with name nihms256229t74.jpg graphic file with name nihms256229t75.jpg OCH3 H H 6.1 ± 0.7 >48
39 graphic file with name nihms256229t76.jpg graphic file with name nihms256229t77.jpg H CH3 H >14.6 ND
40 graphic file with name nihms256229t78.jpg graphic file with name nihms256229t79.jpg H CH3 H >15 ND
41 graphic file with name nihms256229t80.jpg graphic file with name nihms256229t81.jpg H CH3 H >16.8 ND
42 graphic file with name nihms256229t82.jpg graphic file with name nihms256229t83.jpg H CH3 H 12.4 ± 0.6 >51.2
43 graphic file with name nihms256229t84.jpg graphic file with name nihms256229t85.jpg H CH3 H >16.2 ND
44 graphic file with name nihms256229t86.jpg graphic file with name nihms256229t87.jpg H H CH3 3.59 ± 0.36 >60
45 graphic file with name nihms256229t88.jpg graphic file with name nihms256229t89.jpg CH3 H H 3.09 ± 0.55 >67.13
46 graphic file with name nihms256229t90.jpg graphic file with name nihms256229t91.jpg CH3 H H 6.51 ± 0.94 >65
47 graphic file with name nihms256229t92.jpg graphic file with name nihms256229t93.jpg CH3 H H 6.4 ± 0.17 >19.8
48 graphic file with name nihms256229t94.jpg graphic file with name nihms256229t95.jpg CH3 H H 5.8 ±0.36 >117

ND, Not determined