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Table 3 Antiretroviral activity and cytotoxicity of WDO-217 in the anti-HIV

From: A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions

Compound

EC50μM

CC50μM

HIV-1 IIIB

NL4.3/WT

NL4.3/DS5000R

NL4.3/AMD3100R

AZTR

NNRTIRK103N:Y181C

HIV-2 ROD

   

(165)

(>100)

(>30)

(>85)

  

WDO-217

1.04 ± 0.2

0.9 ± 0.05

1.2 ± 0.1

1.7 ± 0.9

1.5 ± 0.6

1.3 ± 0.4

1.04 ± 0.3

75 ± 11

  1. GFP-assay in Jurkat cells.
  2. Values are presented as mean ± std dev from at least 3 independent experiments. Fold resistance of mutant strains towards the respective inhibitor of resistant strains is given in parenthesis (EC50 for NL4.3 wild-type as 1).
  3. EC 50 : 50% effective concentration, concentration of inhibitor required for 50% inhibition of viral replication.
  4. CC 50 : 50% cytotoxic concentration, concentration of inhibitor that kills 50% of the cells.