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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 2.

Enzyme Inhibition and Whole Cell Data of Ethylenediamine-Based FTIs Exhibiting a Range of R2 Sulfonyl Groups

graphic file with name nihms-268901-t0008.jpg
Compound IC50 (nM) Selectivity Processing IC50 (μM)
Number R2 hFTase GGTase-I H-Ras Rap1A
1a
(FTI-2585)		 graphic file with name nihms-268901-t0009.jpg 56 ± 29 2700 ± 2200 48 1.9 ± 1.2 >10
1b
(FTI-2640)		 graphic file with name nihms-268901-t0010.jpg 48 ± 35 4100 ± 1700 85 0.07 >10
1c
(FTI-2644)		 graphic file with name nihms-268901-t0011.jpg 85 ± 0.7 5500 ± 2700 65 NDa ND
1d
(FTI-2592)		 graphic file with name nihms-268901-t0012.jpg 41 ± 26 310 ± 50 7.6 0.3 ± 0.1 >10
1e
(FTI-2589)		 graphic file with name nihms-268901-t0013.jpg 50 ± 13 10,000 200 0.5 ± 0.2 >10
1f
(FTI-2587)		 graphic file with name nihms-268901-t0014.jpg 25 ± 20 820 ± 240 113 0.09 ± 0.06 >10
1g
(FTI-2590)		 graphic file with name nihms-268901-t0015.jpg 30 ± 14 10,000 333 0.6 ± 0.3 >10
1h
(FTI-2591)		 graphic file with name nihms-268901-t0016.jpg 160 ± 110 10,000 63 1.5 ± 0.3 >10
a

ND = not determined.