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Table 1 Anti-proliferative effects of target compounds against tumor cell lines

From: Discovery of novel 2,3,4,5-tetrahydrospiro[benzo[c]azepine-1,1’-cyclohexan]-5-ol derivatives as PARP-1 inhibitors

Compounds

IC50[a](µM)

A549 [b]

OVCAR-3 [c]

HCT-116 [d]

MCF-7 [e]

11a

9.50 ± 1.23

13.61 ± 2.45

10.33 ± 2.74

15.46 ± 2.53

11b

1.95 ± 0.33

4.02 ± 0.24

7.45 ± 1.98

9.21 ± 2.54

11c

4.29 ± 0.56

7.65 ± 2.56

12.57 ± 2.43

7.60 ± 1.96

11d

4.88 ± 1.18

17.14 ± 1.50

8.76 ± 3.11

16.16 ± 3.88

11e

15.61 ± 2.80

7.95 ± 3.35

9.22 ± 4.57

9.33 ± 4.08

11f

11.83 ± 1.07

21.65 ± 8.94

12.21 ± 2.01

8.94 ± 3.17

11 g

6.84 ± 1.68

4.64 ± 0.99

9.81 ± 2.89

7.96 ± 1.10

11 h

15.14 ± 1.18

4.44 ± 0.10

8.97 ± 3.16

6.50 ± 1.78

11i

13.59 ± 2.47

4.28 ± 0.77

10.76 ± 2.95

6.34 ± 3.17

11j

18.82 ± 2.67

5.79 ± 1.25

17.93 ± 1.95

5.27 ± 0.92

11k

12.55 ± 5.91

10.50 ± 0.09

13.05 ± 2.03

7.54 ± 1.05

11 L

11.05 ± 2.98

6.14 ± 0.56

11.72 ± 4.88

8.54 ± 1.65

11 m

8.70 ± 4.10

6.00 ± 1.83

5.87 ± 0.54

9.33 ± 1.33

11n

17.92 ± 3.94

12.61 ± 1.55

15.67 ± 1.98

10.60 ± 0.85

11o

7.40 ± 1.75

4.20 ± 0.48

10.82 ± 2.11

7.99 ± 2.53

11p

9.58 ± 2.53

12.69 ± 1.43

9.93 ± 3.01

16.41 ± 4.37

11q

10.62 ± 1.20

13.18 ± 4.09

> 50

8.72 ± 0.71

11r

11.86 ± 5.74

3.90 ± 0.26

12.08 ± 0.98

> 50

11s

> 50

> 50

> 50

> 50

11t

> 50

> 50

> 50

> 50

11u

> 50

> 50

> 50

> 50

11v

> 50

> 50

> 50

> 50

Rucaparib

4.91 ± 0.11

2.41 ± 0.13

13.51 ± 0.17

12.98 ± 0.28

  1. [a] IC50 values reported as an average ≥ 3 determinations with standard deviation (SD) reported (IC50 = Mean ± SD); [b] human lung adenocarcinoma cell line; [c] human ovarian cancer cell line; [d] human colon cancer cell line; [e] human breast cancer cell line.