Table 3 Cytotoxic activity of target compounds against MCF-7, HCT-116 and HepG-2 cell lines.

From: Targeted potent antimicrobial and antitumor oxygen-heterocyclic-based pyran analogues: synthesis and computational studies

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Compound

R

IC50 (µM)a

Cancerotoxicity

Normotoxicity

MCF-7

HCT-116

HepG-2

HFL-1

WI-38

4a

4-F

12.7 ± 0.05b

14.2 ± 0.01b

1.5 ± 0.01b

–

–

4b

2-Cl

3.9 ± 0.18

8.6 ± 0.25

6.1 ± 0.2

198.6 ± 0.1

171.0 ± 0.2

4c

3-Cl

3.6 ± 0.14

5.5 ± 0.35

3.3 ± 0.5

187.6 ± 0.2

214.1 ± 0.1

4d

4-Cl

8.6 ± 0.29b

6.9 ± 0.97b

0.8 ± 0.08b

164.4 ± 1.1

165.5 ± 1.3

4e

4-Br

4.9 ± 0.25b

2.2 ± 0.58b

1.7 ± 0.13b

189.9 ± 1.1

165.3 ± 1.2

4f

4-I

48.5 ± 0.1

27.8 ± 0.3

39.2 ± 0.2

–

-

4g

2,4-F2

2.7 ± 0.23

6.0 ± 0.11

1.9 ± 0.5

179.4 ± 0.1

190.1 ± 0.3

4h

2,6-F2

60.2 ± 0.3

33.8 ± 0.12

48.1 ± 0.2

–

–

4i

2,3-Cl2

2.3 ± 0.01

3.5 ± 0.15

2.8 ± 0.17

154.5 ± 0.1

160.1 ± 0.2

4j

2,4-Cl2

2.0 ± 0.02

5.8 ± 0.16

14.1 ± 0.18

180.8 ± 0.3

177.8 ± 0.3

4k

2,5-Cl2

6.6 ± 0.4

2.5 ± 0.23

1.8 ± 0.03

–

–

4l

2,6-Cl2

12.1 ± 0.06

21.3 ± 0.01

2.3 ± 0.02

–

–

4m

3,4-Cl2

1.3 ± 0.21

2.3 ± 0.97

1.8 ± 0.06

181.0 ± 0.1

175.5 ± 0.2

4n

3,5-Br2-2-OMe

1.4 ± 0.05

1.2 ± 0.06

5.6 ± 0.21

139.5 ± 0.1

135.4 ± 0.3

4o

2,3,4-(OMe)

55.3 ± 0.01

35.9 ± 0.02

17.6 ± 0.05

–

–

4p

3,4,5-(OMe)

114.4 ± 0.03

91.4 ± 0.01

106.5 ± 0.1

–

–

4q

2,3,5-Cl3

110.4 ± 0.1

107.2 ± 1.6

76.5 ± 0.9

–

–

Erlotinib

–

4.16 ± 0.2

11.21 ± 0.6

8.19 ± 0.4

14.0 ± 1.2

28.5 ± 0.2

  1. aIC50 values expressed in µM as the mean values of triplicate wells from at least three experiments and are reported as the mean ± standard error andb 25.
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