Table 2 Cytotoxicities of the synthetic metabolites of CB 1954 (1) and SN 23862 (7) against NTR−ve cell lines

From: 2-Amino metabolites are key mediators of CB 1954 and SN 23862 bystander effects in nitroreductase GDEPT

 

IC50 (μ M) following 4 h drug exposure

Cmpd

SiHa

WiDr

V79puro

AA8

UV4

AA8/UV4a

1

277±36

485±34

2950±113

2480±260

135±28

22.1±5.2

(CB 1954)

      

2

n.d.b

n.d.

n.d.

22

6.3

3.4

3

7.9±3.3

21±3

56±7

28±8

3.7±0.7

7.1±1.0

4

45±9

26±5

6.9±0.6

39±6

0.62±0.05

63±5

5

163±39

141±34

238±6

62±12

47±5

1.2±0.1

7

>800

>1000

>500

ca1000c

761±89

ca 1.3

(SN 23862)

      

8

2.07±0.08

1.2±0.1

1.74±0.23

2.3±0.1

0.045±0.001

51±1

9

2.5±1.1

2.75±0.15

3.94±0.19

8.8±1.1

0.23±0.04

40±4

  1. Values are mean±s.e.m. for 2–15 (median 4) independent experiments.
  2. aIntra-experiment IC50 ratio.
  3. bNot determined.
  4. cIC50 above the solubility limit in some experiments.