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. Author manuscript; available in PMC: 2019 Jun 25.
Published in final edited form as: Eur J Med Chem. 2018 May 12;154:367–391. doi: 10.1016/j.ejmech.2018.04.062

Table 3.

Inhibitory activity against Cell-to-Cell HIV transmission by NBD compounds.

A. Chronically infected cells H9-HIV-1IIIB and Molt-HIV-1ADA were used as donor cells and TZMb-l were used as acceptor cells.
Compound IC50 (μM)a
TZMb-l/H9-HIV-1IIIB TZMb-l/Molt-HIV-1ADA
NBD-14107 0.56±0.03 1.7±0.1
48 0.41±0.07 1±0.1
39 0.079±0.003 0.44±0.002
55 0.097±0.006 0.3±0.02
BMS-626529 0.025±0.005 ~0.4
B. PBMC cells acutely infected with lab-adapted and primary clinical isolates HIV-1 were used as donor cells and TZMb-l were used as acceptor cells.
Viral Strain Subtype/coreceptor IC50 (μM)a
NBD-14107 48 39 55 BMS-626529
HIV-193RW018 A / R5 2.5±0.1 2.4±0.3 0.2±0.006 0.18±0.01 ~0.1
HIV-193RW034 A / R5 0.89±0.07 0.87±0.01 0.29±0.02 0.19±0.01 ~0.1
HIV-1LAIb B / X4 0.73±0.03 0.31±0.01 0.21±0.05 0.26±0.05 ~0.1
HIV-189.6b B / R5X4 2.6±0.3 0.54±0.1 0.25±0.004 0.33±0.01 ~0.1
HIV-1BaLb B / R5 0.64±0.1 0.45±0.03 0.23±0.01 0.33±0.02 ~0.1
HIV-192US073 B / R5 1.2±0.05 0.66±0.05 0.22±0.01 0.16±0.001 ~0.1
HIV-192US657 B / R5 3.6±0.2 1.2±0.08 0.59±0.05 0.71±0.03 ~0.1
HIV-193BR019 BF/ X4 1.9±0.16 0.25±0.04 0.31±0.01 0.2±0.006 ~0.1
HIV-1CMU02 EA / X4 4.5±0.3 4.2±0.5 1.87±0.01 1.1±0.14 >6
HIV-1Ru132 G / R5 0.84±0.1 0.57±0.03 0.33±0.1 0.3±0.02 ~0.1
HIV-1RU570 G / R5 1.3±0.1 0.28±0.006 0.37±0.004 0.32±0.01 ~0.1
HIV-1BCF01 O / R5 0.96±0.06 0.31±0.03 0.28±0.06 0.22±0.01 >6
HIV-1BCF03 O / R5 2.2±0.06 0.71±0.05 1.6±0.08 0.18±0.01 >6
Mean ± SEM (μM): (n=13) 1.84±0.3 0.98±0.3 0.52±0.15 0.34±0.07 -
Toxicity in-infected PBMC : CC50 (μM) >60 ~61 ~61 38.7±3.8 >10
a

The reported IC50 values represent the means ± standard deviation (SD), n=3.

a

The reported IC50 values represent the means ± standard deviation (n = 3).

b

Laboratory-adapted virus; all the rest are clinical isolate viruses