. Author manuscript; available in PMC: 2009 Jan 15.

Published in final edited form as: Bioorg Med Chem Lett. 2007 Dec 3;18(2):494–497. doi: 10.1016/j.bmcl.2007.11.104

Table 2.

Inhibition of rat PFT and protein geranylgeranyltranferase-I (PGGT-I) by 2-oxo-tetrahydro-1,8-naphthyridine-based PFTIs

Compd.	Rat PFT, % inh. at the indicated inhibitor concentration (nM)¹					Rat PGGT-I, % inh. at 1 µM inhibitor²
	5000	500	50	5	0.5
16	51	8	8	5	0	16
17	39	0	1	0	0	0
18	47	9	0	0	0	0
20	85	71	28	7	0	5

PFT assays were carried out as in Ref. 7.

PGGT-I assays carried out as for PFT assays except rat PGGT-I (5 ng), 5 µM H-Ras-CVLL and 0.65 µM [³H]geranylgeranyl pyrophosphate were used (8).