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Table 1 Structures, preparative yields (from 3), and DU-145 proliferation inhibition data of compounds 2a-s.

From: Discovery and SAR exploration of N-aryl-N-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer

Compound

R1

R2

Yield, %

IC50, μMa

2a b

62

2.2 ± 0.30

2b

68

0.86 ± 0.10

2c

70

1.6 ± 0.25

2d

29

2.6 ± 0.35

2e

43

1.0 ± 0.01

2f

43

1.0 ± 0.12

2g

73

2.7 ± 0.22

2h

37

1.6 ± 0.14

2i

77

0.64 ± 0.025

2j

56

0.55 ± 0.010

2k

81

0.084 ± 0.005

2l

54

2.7 ± 0.50

2m

46

0.96 ± 0.08

2n

72

0.93 ± 0.009

2o

75

1.8 ± 0.30

2p

82

2.1 ± 0.17

2q

65

0.91 ± 0.07

2r

66

1.5 ± 0.09

2s

55

0.38 ± 0.024

  1. aIC50 values have been evaluated for standard error. The values reported are the mean of 2 determinations, standard error provided.
  2. bCompound 2a reffered in this table is indetical with the hit compound 1 in the text and figure 1.