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. Author manuscript; available in PMC: 2011 Feb 26.
Published in final edited form as: J Med Chem. 2010 Oct 14;53(19):6867–6888. doi: 10.1021/jm1001748

Table 4.

Enzyme Inhibition and Whole Cell Data of Ethylenediamine-Based FTIs Exhibiting a Range of para-Substituted Anilines

graphic file with name nihms-268901-t0045.jpg
compd
 IC50 (nM)
 processing IC50 (nM)
no. X hFTase GGTase-I selectivity H-Ras Rap1A
4 (FTI-2586) Br 79 ± 30 530 ± 170 6.7 1.6 ± 1.3 >10
1a (FTI-2585) CN 56 ± 29 2700 ± 2200 48 1.9 ± 1.2 >10
11 (FTI-2720) CO2tBu 5400 (n = 2) 4900 (n = 2) 0.9 ND ND
12 (FTI-2721) COOH > 10000 > 10000 – ND ND
13 (FTI-2728) CONH2 5300 (n = 2) > 10000 > 2 ND ND
14 (FTI-2727) Ph 6850 (n = 2) 5000 ± 2600 0.7 ND ND