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. Author manuscript; available in PMC: 2014 Feb 28.
Published in final edited form as: J Med Chem. 2013 Feb 12;56(4):1573–1582. doi: 10.1021/jm3013882

Table 2.

Structure activity of C-terminal Partial Ligand Alternatives

graphic file with name nihms445567u2.jpg
SCCP R1 X R2 R3 R4 R5 CDK2/cyclin A
IC50 (μM)		 CDK4/cyclin D1
IC50 (μM)
5807 4-chloro C H H H H 106.1±26.2 >200
5824 4-chloro N H F H H 53.2±11.6 >200
5823 4-chloro N H H F H 18.1±4.0 >200
5822 4-chloro N H H Cl H 54.4±0.9 >500
5825 4-chloro N CH3 H H H 60±3.5 >500
5848 3,5-dichloro N H Cl H H 61±10.8 120
5849 3,5-dichloro C H Cl H Cl >180 120
5926 3,5-dichloro N H F F H >180 >180