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. Author manuscript; available in PMC: 2016 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2015 Sep 25;23(21):6974–6992. doi: 10.1016/j.bmc.2015.09.036

Table 1.

Inhibitory Activity of Benzoylbenzophenone Thiosemicarbazone Analogues

graphic file with name nihms-730300-f0014.jpg
IC50a Values (nM)
Cmpd R1 R2 R3 R4 X Cat L Cat B
1 H H H H C=O 9.9 >10000
2 H H H Bz C=O 56.0 >10000
4 H H H H CH(OH) 23.8 >10000
8 F H H H C=O 14.4 >10000
9 Br H H H C=O 1522 >10000
10 Br H H H C=NNHC(S)NH2 >10000 >10000
11 OCH3 H H H C=O 5117 >10000
13 OH H H H C=O 340 >10000
14 OCH(CH3)2 H H H C=O >10000 >10000
20 H CH3 H H C=O 654 >10000
22 H Br H OH C=O ~10000b >10000
31 H OH H Br C=O 71.6 >10000
32 H H F Br C=O 8.1 >10000
33 H Br H Br C=O 10347 >10000
a

These values are averages of a minimum of a triplicate of experiments. Each assay utilized 2% DMSO with a 5 min pre-incubation period. Standard error values can be found in the Supplementary data.

b

Compound 22 inhibited cathepsin L activity by 56.9% at 10000 nM.