Skip to main content
. Author manuscript; available in PMC: 2018 Oct 15.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Sep 13;27(20):4614–4621. doi: 10.1016/j.bmcl.2017.09.022

Table 2.

Screening data for basic cyclic amides 38–66.

Ar Cmpd R1 & R2 CC50 (μM)
HT29 PC3 MDA-MB-231
graphic file with name nihms907144t1.jpg 38 graphic file with name nihms907144t7.jpg 1.81±0.06 5.27±0.32 3.78±0.26
39 graphic file with name nihms907144t8.jpg 1.65±0.14 5.36±0.18 5.42±0.24
40 graphic file with name nihms907144t9.jpg 2.98±18.68 6.66±0.43 7.66±0.52
41 graphic file with name nihms907144t10.jpg 1.41±0.04 4.33±0.23 3.75±0.23
42 graphic file with name nihms907144t11.jpg 1.16±0.08 4.64±0.23 3.72±0.23
43 graphic file with name nihms907144t12.jpg 1.55±0.06 5.10±0.36 4.16±0.29
44 R1, R2 = -(-CH2CH2-)2NCH2CH2CH2N(CH3)2 1.69±0.08 4.28±0.16 3.77±1.18
45 R1, R2 = -(-CH2CH2-)2NCH2CH2N(CH3)2 2.17±0.06 6.23±0.37 4.05±0.23
46 R1, R2 = -(-CH2CH2-)2N(pyridin-4-yl) 1.13±0.07 2.76±0.19 3.08±0.07
47 R1, R2 = -(-CH2CH2-)2CH(pipyridin-1-yl) 1.06±0.05 4.06±0.27 2.61±0.09
48 graphic file with name nihms907144t13.jpg 1.64±0.07 4.45±0.16 4.10±0.19
49 graphic file with name nihms907144t14.jpg 4.29±0.19 13.42±0.49 11.50±0.53
50 graphic file with name nihms907144t15.jpg 2.94±0.16 7.35±0.32 7.21±0.22
51 graphic file with name nihms907144t16.jpg 2.47±0.67 6.50±0.84 3.69±0.17

graphic file with name nihms907144t2.jpg 52 R1, R2 = -(-CH2CH2-)2NCH2CH2CH2N(CH3)2 23.75±1.48 >50.00 46.18±2.63
53 R1, R2 = -(-CH2CH2-)2N(Pyridin-4-yl) 9.20±0.39 21.93±2.16 22.74±2.29
54 R1, R2 = -(-CH2CH2-)2CH(pipyridin-1-yl) >50.00 >50.00 >50.00
55 graphic file with name nihms907144t11.jpg 19.03±1.26 >50.00 >50.00
56 graphic file with name nihms907144t12.jpg 20.16±1.06 >50.00 >50.00

graphic file with name nihms907144t3.jpg 57 graphic file with name nihms907144t7.jpg 13.39±0.71 46.49±5.98 41.09±3.78
58 graphic file with name nihms907144t8.jpg 4.18±0.19 9.62±0.66 10.38±0.59
59 R1, R2 = -(-CH2CH2-)2N(Pyridin-4-yl) 2.79±0.13 5.45±0.68 6.50±0.77
60 graphic file with name nihms907144t12.jpg 4.22±0.15 12.28±0.72 11.14±0.56

graphic file with name nihms907144t4.jpg 61 graphic file with name nihms907144t7.jpg 1.21±0.04 4.94±0.28 3.56±0.28
62 R1, R2 = -(-CH2CH2-)2NCH2CH2CH2N(CH3)2 1.62±0.06 4.21±0.23 2.90±0.07
63 R1, R2 = -(-CH2CH2-)2N(Pyridin-4-yl) 5.25±0.20 12.28±0.37 7.71±1.5
64 graphic file with name nihms907144t11.jpg 1.66±0.04 7.72±0.45 5.58±0.33
65 graphic file with name nihms907144t12.jpg 1.58±0.04 4.25±0.15 3.61±0.23

graphic file with name nihms907144t5.jpg 66 graphic file with name nihms907144t7.jpg 2.68±0.12 10.19±0.41 7.19±0.31