. 2016 Nov 28;8(1):90–95. doi: 10.1021/acsmedchemlett.6b00392

Table 1. SAR Studies: Substituents on Ring A^a.

graphic file with name ml-2016-003924_0006.jpg

compd	R¹	R²	R³	EC₅₀ (μM)
1	H	H	H	10
2	C(O)NH₂	H	H	>100
3	H	C(O)NH₂	H	9.2
4	H	H	C(O)NH₂	42
5	H	C(O)NHMe	H	6.2
6	H	C(O)N(Me)₂	H	6.4
7	H	C(O)NHEt	H	11
8	H	C(O)NHⁱPr	H	8.9
9	H	C(O)NHPh	H	6.4
gemcitabine				0.0015
erlotinib				27
3 mA				>100
chloroquine				14
spautin-1				20

EC₅₀ values were determined in triplicate in MIA PaCa-2 cells.

Table 1. SAR Studies: Substituents on Ring Aa.