. Author manuscript; available in PMC: 2009 Sep 21.

Published in final edited form as: J Med Chem. 2008 Aug 5;51(16):5052–5063. doi: 10.1021/jm8003366

Table 2.

IC₅₀s for pyrrolopyrimidine compounds 1–5 in in vitro and in situ GARFTase inhibition assays.

Antifolate	IC₅₀

	In vitro (µM)	In situ (nM)

1	>20	>1000
2	2.44 (0.12)	18(2.0)
3	0.15 (0.01)	6.8(0.9)
4	2.26 (0.16)	7.2(1.8)
5	2.51 (0.25)	8.6(0.7)
Pemetrexed	>20	30(7.7)
Lometrexol	0.78 (0.08)	14(5.6)

GARFTase inhibition assays, both in vitro and in situ, were performed as described in the Experimental Section. The IC₅₀ data shown are mean values from 3 (in vitro; SEM in parentheses) or 2 (in situ; range in parentheses) experiments.