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. Author manuscript; available in PMC: 2020 May 23.
Published in final edited form as: Chem Biol Drug Des. 2019 Dec 19;95(3):388–393. doi: 10.1111/cbdd.13650

Table 1.

Effects of compounds 5a-qand 1on CHOP-Luc reporter and β cell viability against (tunicamycin) Tm

graphic file with name nihms-1589292-t0002.jpg
CompoundID R1 R2 R3 Max Activity (%)a EC50 (μM)b
1c 3-Cl,2-Me - 2,5-di Me 97 6 ± 1
5a 3-Cl,2-Me H 2,5-di Me 45 18 ± 4
5b 3-Cl,2-Me H 2-Pyridine 16 38 ± 9
5c 3-Cl,2-Me H Indazole Cytotoxic -
5d 3-Cl,2-Me H 4-OMe 55 32 ± 7
5e 3-Cl,2-Me H 4-SO2NH2 52 40 ± 12
5f 3-Cl,2-Me H Tyramine 41 34 ± 8
5g 3-Cl,2-Me H 4-CF3 88 13 ± 1
5h 3-Cl,2-Me H 3-OMe,4-OH 100 10 ± 2
5i 3-Cl,2-Me H 3-CF3 46 32 ± 7
5j H H 4-CF3 35 43 ± 11
5k 4-Et H 4-CF3 42 45 ± 8
5l 4-F H 4-CF3 12 41 ± 6
5m (WO5m) 3-OH H 4-CF3 100 0.1 ± 0.01
5n 3-OH H 3-OMe,4-OH 30 65 ± 8
5o 3-OMe,4-OH H 4-CF3 43 29 ± 6
5p 3-Cl,2-Me Me 4-CF3 34 63 ± 4
5q 3-Cl,2-Me Tyrosine 4-CF3 Cytotoxic -
a

Maximum activity value is reported as % rescue from Tm (0.15 μg/mL) -induced reduction of cell viability, as measured by intracellular ATP levels; the values for Tm treatment alone and control (DMSO, without Tm) treatment are designated as 0% and 100%, respectively.

b

EC50 values (the concentrations that reach half-maximal activity) for INS-1 cell viability are calculated with GraphPad Prism from the data of ten 2-fold serial titration points in all tables. All experiments were performed in triplicate.

c

Compound 1 contains the 1,2,3-triazole group, as shown in Figure 1.