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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 7.

Enzyme Inhibition and Whole Cell Data of Optimized, Ethylenediamine-Based FTIs

graphic file with name nihms-268901-t0064.jpg
Compound IC50 (nM) Selectivity Processing IC50 (μM)
Number R2 R3 R4 hFTase GGTase-I H-Ras Rap1A
1a
(FTI-2585)		 graphic file with name nihms-268901-t0065.jpg graphic file with name nihms-268901-t0066.jpg graphic file with name nihms-268901-t0067.jpg 56 ± 29 2700 ± 2200 48 1.9 ± 1.2 >10
1ax
(FTI-2602)		 graphic file with name nihms-268901-t0068.jpg graphic file with name nihms-268901-t0069.jpg graphic file with name nihms-268901-t0070.jpg 60 ± 10 530 ± 120 8.8 0.1 ±0.07 >10
1f
(FTI-2587)		 graphic file with name nihms-268901-t0071.jpg graphic file with name nihms-268901-t0072.jpg graphic file with name nihms-268901-t0073.jpg 25 ± 20 820 ± 240 33 0.09 ± 0.06 >10
21a
(FTI-2736)		 graphic file with name nihms-268901-t0074.jpg graphic file with name nihms-268901-t0075.jpg graphic file with name nihms-268901-t0076.jpg 400 ± 160 610 ± 160 1.5 0.268 ± 0.212 6.2 ± 1.2
21b
(FTI-2734)		 graphic file with name nihms-268901-t0077.jpg graphic file with name nihms-268901-t0078.jpg graphic file with name nihms-268901-t0079.jpg 250 ± 190 520 ± 90 2.1 0.0887 ± 0.0258 2.7 ±1.5
21c
(FTI-2735)		 graphic file with name nihms-268901-t0080.jpg graphic file with name nihms-268901-t0081.jpg graphic file with name nihms-268901-t0082.jpg 350 ± 170 690 ± 92 2 0.288 ± 0.251 19