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. Author manuscript; available in PMC: 2006 Jan 25.
Published in final edited form as: Biochem Pharmacol. 2003 Nov 1;66(9):1755–1768. doi: 10.1016/s0006-2952(03)00542-2

TABLE 1.

Compound classes and activity in K562 γYAC transcription assays, K562 cytotoxicity assay (MTT) K562 HbF e.l.i.s.a. and human primary progenitor HbF e.l.i.s.a.

Side chains Transcription (24hr) Cytotoxicity (48hr) Maximum HbF increase (4 day)
Compound ID/ Structural Class Y X EC50 (uM) Maximum Induction IC50 (uM) K562 cells Human progenitor cells
Inline graphic
OSI-2040 		0.15 4.3 0.5 5.4 (0.1uM) 4.5 (0.04uM)
graphic file with name nihms3499f7.jpg
OSI-168961 1-hydroxy 2-napthyl 2-chloro-4-nitro 0.1 3.2 >50 2.8 (2uM) 2.4 (0.8uM)
OSI-168996 1-hydroxy 4-chloro 2-napthyl 4-cyano 1 3.8 30 3.8 (0.7uM) 2.4 (0.8uM)
OSI-97345 3-methylbenzo[b] thiophene 4-methyl 5.0 3.6 >50 2 (15uM) 4.1 (4uM)
graphic file with name nihms3499f8.jpg
OSI-168992 cyclohexyl 2-nitro 1.0 2.0 >20 3.1 (20uM) 2.6 (0.8uM)
graphic file with name nihms3499f9.jpg
OSI-169055 <> 1-benzyl-1H- pyrrolo(1,2- A)imidazol-5-yl)- <0.1 2.2 >50 2.1 (20uM) nd
graphic file with name nihms3499f10.jpg
OSI-101820 4-bromo 3-nitro 8.0 3.3 >50 2.1 (13uM) 4.7 (4uM)
graphic file with name nihms3499f11.jpg
OSI-169170 hydroxy 4-methoxyphenyl 8.0 5.8 >50 3.2 (2uM) 7.2 (20uM)
graphic file with name nihms3499f12.jpg
OSI-22121 2,3 propylene <> 3.5 2.6 30 5.4 (25uM) 2.1 (0.8uM)
graphic file with name nihms3499f13.jpg
OSI-169040 3(2-keto indolyl) <> 9.0 2.9 >50 2 (20uM) nd
graphic file with name nihms3499f14.jpg
OSI-102695 <> <> 0.9 2.5 >20 1.7 (20uM) 3.5 (4uM)
graphic file with name nihms3499f15.jpg
OSI-169050 <> <> 0.4 3.0 >50 2.3 (6 uM) 1.5 (20uM)
aza-cytidine 0.6 2.5 1 3.1 (1uM) 10 (1uM)
hydroxyurea na 1.2 nd 2.8 (200uM) 5.9 (100uM)