Table 1 Structure–activity relationship (SAR) of NAIMS (3a—3 h).

From: Anti-cancer Effects of 1,4-Dialkoxynaphthalene-Imidazolium Salt Derivatives through ERK5 kinase activity inhibition

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R1

R2

IC50 Viabilitya (µM)

Inhibition of PCNA expressionb (%)

3a

Isoamyl

Me

13.7 ± 2.4

30.0 ± 1.9

3b

Isoamyl

Isoamyl

10.1 ± 3.1

40.0 ± 2.0

3c

Isoamyl

Bn

15.0 ± 0.8

71.7 ± 2.9

3d

Isoamyl

Me

13.9 ± 0.7

51.6 ± 1.4

3e

Isoamyl

Bn

14.8 ± 2.1

0 ± 3.3

3f.

Me

Isoamyl

17.0 ± 1.9

0 ± 2.8

3g

i-Pr

Isoamyl

12.9 ± 1.8

29.3 ± 4.3

3h

n-Octyl

Isoamyl

14.3 ± 1.1

51.7 ± 5.4

  1. aIC50 values were determined from MTT-based cell proliferation assays. bPCNA expressions were determined by quantitative RT-PCR. .
  2. *IC50 and PCNA expression values expressed as mean ± SD.
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