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. 2020 Jun 17;11(7):1421–1428. doi: 10.1021/acsmedchemlett.0c00105

Table 1. Cytotoxic Activities of 2,4-Diaminopteridine Derivatives on HeLa Cancer Cells and Ect1/E6E7 Normal Cells with (4 Gy) or without (0 Gy) X-rays by MTT Assay.

  IC50 (μM)
  2a 2b 2c 2d 2e 2f MTX
HeLa + 0 Gy 2.1 ± 0.2 >80 9.8 ± 0.3 32.6 ± 1.2 24.5 ± 1.2 4.6 ± 0.3 1.5 ± 0.2
HeLa + 4 Gy 0.64 ± 0.03 >80 6.3 ± 0.2 14.8 ± 0.4 14.6 ± 0.8 2.3 ± 0.2 0.82 ± 0.08
SERa 3.3 ± 0.2 NA 1.6 ± 0.1 2.20 ± 0.2 1.7 ± 0.1 2.0 ± 0.4 1.8 ± 0.3
Ect1/E6E7 + 0 Gy 6.9 ± 0.3 >80 20.0 ± 1.0 59.3 ± 1.6 40.1 ± 1.6 10.9 ± 1.8 2.9 ± 0.3
Ect1/E6E7 + 4 Gy 3.1 ± 0.2 >80 13.9 ± 1.0 38.1 ± 1.9 19.8 ± 1.2 5.3 ± 0.3 1.8 ± 0.2
SERb 2.2 ± 0.1 NA 1.4 ± 0.2 1.6 ± 0.1 2.0 ± 0.1 2.1 ± 0.2 1.6 ± 0.3
SI0c 3.3 ± 0.4 NA 2.0 ± 0.1 1.8 ± 0.1 1.6 ± 0.1 2.5 ± 0.3 1.9 ± 0.2
SI4d 4.8 ± 0.5 NA 2.2 ± 0.1 2.6 ± 0.1 1.4 ± 0.1 2.3 ± 0.4 2.2 ± 0.1
a

Sensitivity enhancement ratio (SER) = IC50(HeLa + 0 Gy)/IC50(HeLa + 4 Gy).

b

SER = IC50 (Ect1/E6E7 + 0 Gy)/IC50 (Ect1/E6E7 + 4 Gy).

c

Safe index for 0 Gy (SI0) = (Ect1/E6E7 + 0 Gy)/(HeLa + 0 Gy).

d

Safe index for 4 Gy (SI4) = (Ect1/E6E7 + 4 Gy)/(HeLa + 4 Gy).