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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 5.

Enzyme Inhibition and Whole Cell Data of Ethylenediamine-Based FTIs Exhibiting a Range of R4 Anilines

graphic file with name nihms-268901-t0047.jpg
Compound IC50 (nM) Selectivity
Number R4 hFTase GGTase-I
1az
(FTI-2722)		 graphic file with name nihms-268901-t0048.jpg 510 ± 62 >10,000 >20
19a
(FTI-2718)		 graphic file with name nihms-268901-t0049.jpg 550 ± 110 >10,000 >18
19b
(FTI-2733)		 graphic file with name nihms-268901-t0050.jpg 520 ± 320 >10,000 >19
19c
(FTI-2707)		 graphic file with name nihms-268901-t0051.jpg 110 ± 26 >10,000 >91
19d
(FTI-2709)		 graphic file with name nihms-268901-t0052.jpg 620 ± 100 >10,000 >16
19e
(FTI-2712)		 graphic file with name nihms-268901-t0053.jpg 230 ± 110 9400 (n = 2) 41
19f
(FTI-2713)		 graphic file with name nihms-268901-t0054.jpg 64 ± 8.6 >10,000 >156
I9g
(FTI-2715)		 graphic file with name nihms-268901-t0055.jpg 290 ± 180 >10,000 >34
19h
(FTI-2719)		 graphic file with name nihms-268901-t0056.jpg 490 ± 70 8750 ± 750 18