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. Author manuscript; available in PMC: 2017 Apr 19.
Published in final edited form as: ChemMedChem. 2016 Mar 30;11(8):850–861. doi: 10.1002/cmdc.201600021

Table 4.

Phenotypic screening of R1 analogs in CML cell lines.

graphic file with name nihms800395u5.jpg
Compound ID R R1 IC50 AR230 (μm) IC50 AR230R (μm) LogP[a]
RG1-066 3-pyridyl c-Pent >32 >32 3.61
RG1-085 2-pyridyl c-Pent >32 >32 3.61
AM1-116 4-fluoro-3-pyridyl c-Pent >32 >32 3.74
AM1-117 4-fluoro-2-pyridyl c-Pent >32 >32 3.74
AM1-020 2,3,5,6-tetrafluoro-phenyl c-Pent >32 13.1 4.28
AM1-112 4-chloro-2,3,5,6-tetrafluorophenyl c-Pent >32 30.7 4.6
AM1-077 4-bromo-2,3,5,6-tetrafluorophenyl c-Pent 25.07 20.3 4.74
AM1-066 4-trifluoromethyl-2,3,5,6-tetrafluorophenyl c-Pent 20.4 21.6 4.84
AM1-030 4-methyl-2,3,5,6-tetrafluorophenyl c-Pent >32 18.6 4.54
AES1-094 4-fluorophenyl t-Bu >32 10.6 1.96
[a]

Values calculated by StarDrop.