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. 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 4.

Screening data for neutral amides 72–86.

Ar Cmpd R1 & R2 CC50 (μM)
HT29 PC3 MDA-MB-231
graphic file with name nihms907144t1.jpg 72 R1 = H, R2 = benzyl 1.52±0.39 16.36±8.55 3.61±1.87
73 R1 = H, R2 = furan-2-ylmethyl 2.08±0.82 12.98±6.83 3.40±1.07
74 R1 = H, R2 = thiophen-2-ylmethyl 2.16±0.71 11.03±5.95 5.66±2.69
75 R1 = H, R2 = -CH2CH2CH(CH3)2 >50.00 >50.00 >50.00
76 R1 = H, R2 = D-Alanine methyl ester 16.22±2.61 44.18±7.38 31.99±2.33
77 R1 = H, R2 = L-Alanine methyl ester 23.92±1.92 >50.00 38.86±6.04
78 R1 = H, R2 = L-Histidine methyl ester 23.01±3.09 >50.00 >50.00

graphic file with name nihms907144t2.jpg 79 R1 = H, R2 = benzyl 0.50±0.23 2.64±1.19 0.78±0.32
80 R1 = H, R2 = furan-2-ylmethyl 1.00±0.50 >50.00 2.73±1.21
81 R1 = H, R2 = -CH2CH2CH(CH3)2 17.65±1.11 20.23±2.29 27.72±3.37

graphic file with name nihms907144t3.jpg 82 R1 = H, R2 = -CH2CH2CH(CH3)2 5.24±1.18 8.20±1.92 8.73±1.97

graphic file with name nihms907144t4.jpg 83 R1 = H, R2 = benzyl 23.56±2.04 >50.00 19.63±2.98
84 R1 = H, R2 = furan-2-ylmethyl 5.48±1.70 26.44±15.80 6.70±2.23
85 R1 = H, R2 = -CH2CH2CH(CH3)2 >50.00 >50.00 24.20±5.35

graphic file with name nihms907144t5.jpg 86 R1 = H, R2 = benzyl 2.14±0.46 5.71±1.75 3.68±1.10