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Table 1 Structure and activity of IN-LEDGF inhibitors designed in this study

From: Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage

Compound

Structure

MW (g/mol)

Biochemical assays

MT4 assays

CCD-IBD IC50(μM)

IN-LEDGF IC50(μM)

IN ST IC50(μM) plateau (%)

NL4-3 EC50(μM)

HxB2 EC50(μM)

CC50(μM)

Mut029*

391

1.7

2.5

NT

3.8

3.8

>50

Mut047*

390

3.8

7.9

0.88 70%

16

19

>50

Mut049

355

18

3.5

0.18 56%

2.0

0.75

>50

Mut062*

394

2.7

3.1

0.54 73%

3.3

1.3

>50

Mut063

433

>100

>100

>100 ND

>50

NT

>50

Mut075

353

14

4.0

NT

3.4

1.0

>50

Mut101*

410

0.23

0.20

0.17 66%

0.54

0.092

>50

  1. Structure, molecular weight, and activities of compounds. NT = not tested. *compounds that have been co-crystallized with IN-CCD; IC50 = concentration required to inhibit CCD-IBD interaction, IN-LEDGF interaction or IN strand transfer activity by 50%; EC50 = concentration required to inhibit HIV-1 infection of MT4 cells by 50%; CC50 = concentration required to inhibit MT4 cell viability by 50%.
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Retrovirology

ISSN: 1742-4690

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