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. 2013 May 16;21(14):4151–4157. doi: 10.1016/j.bmc.2013.05.009

Table 1.

Anti-HCMV activity of the synthesized compounds in HEL cell cultures.

graphic file with name fx2.jpg

Compd R1 R2 n mp (°C) Yield (%) EC50 (μМ)a
Cytotoxicity (μМ)
AD-169 Davis Cell morphology (MCC)b Cell growth (CC50)c
9 H H 3 151–153 88 >100 >100 >100 >100
10 H 2-Me 3 147–149 72 >100 >100 >100 >100
11 H 3-Me 3 101–103 75 45.0 55.0 >100 >100
12 H 4-Me 3 146–147 87 >20 >20 100 >100
13 H 3,5-Me2 3 96–98 85 >100 >100 >100 >100
14 H 4-iPr 3 139–140 78 25.0 15.0 100 >100
15 H 4-tBu 3 125–127 77 14.0 12.0 100 40
16 H 4-Ph 3 174–175 76 >20 54 100 ND
17 H 4-CN 3 185–186 84 8.9 5.5 100 100
18 H 4-CO2nPr 3 131–132 76 45.0 45.0 ⩾100 >100
19 H 4-Cl 3 168–169 84 >100 >100 >100 ND
20 H 4-Br 3 125–127 76 9.4 12.0 100 >100
21 H 4-NO2 3 197–199 78 >4 >4 20 ND
22 Br 4-Br 3 160–162 77 36.0 67.0 >100 >100
23 I 4-Br 3 166–168 78 13.0 20.0 ⩾100 >100
24 Me 4-Br 3 169–171 82 8.9 9.0 100 >100
25 H 4-Br 1 179–181 79 >100 >100 >100 ND
26 H 4-Br 2 143–144 80 >20 >20 100 ND
27 H 4-Br 4 121–122 70 >4 >4 20 ND
28 H 4-Br 6 145–147 76 12.0 8.9 ⩾100 >100
29 H 4-CO2H 3 225–227 81 >100 >100 >100 ND
30 H 4-NH2 3 190–192 59 55.0 55.0 >100 >100
Ganciclovir 7.0 8.3 394 200
Cidofovir 1.3 1.1 317 161
a

Effective concentration required to reduce virus plaque formation by 50%. Virus input was 100 plaque forming units (PFU).

b

Minimum cytotoxic concentration that causes a microscopically detectable alteration of cell morphology.

c

Cytotoxic concentration required to reduce cell growth by 50%.