Skip to main content
. 2018 Mar 27;8(22):11871–11885. doi: 10.1039/c8ra01440j

Inhibitory effects of compounds 3a–3o against CDK2/cyclin A and CDK9/cyclin T1.

graphic file with name c8ra01440j-u12.jpg
Compd. R3 R4 R5 IC50a (μM)
CDK2/cyclin A CDK9/cyclin T1
2e H H graphic file with name c8ra01440j-u13.jpg 0.24 ± 0.04 0.095 ± 0.004
3a H H graphic file with name c8ra01440j-u14.jpg 1.10 ± 0.15 0.48 ± 0.22
3b H H graphic file with name c8ra01440j-u15.jpg 0.38 ± 0.06 0.08 ± 0.001
3c H H graphic file with name c8ra01440j-u16.jpg 0.30 ± 0.07 0.065 ± 0.023
3d H H graphic file with name c8ra01440j-u17.jpg 0.13 ± 0.02 0.66 ± 0.02
3e H H graphic file with name c8ra01440j-u18.jpg 0.75 ± 0.14 0.23 ± 0.01
3f F H graphic file with name c8ra01440j-u19.jpg NDb ND
3g H F graphic file with name c8ra01440j-u20.jpg 0.083 ± 0.035 0.10 ± 0.01
3h OCH3 H graphic file with name c8ra01440j-u21.jpg ND ND
3i H OCH3 graphic file with name c8ra01440j-u22.jpg 0.57 ± 0.08 0.19 ± 0.02
3j H CH3 graphic file with name c8ra01440j-u23.jpg 2.90 ± 0.06 0.16 ± 0.02
3k H graphic file with name c8ra01440j-u24.jpg H 0.44 ± 0.04 0.083 ± 0.002
3l graphic file with name c8ra01440j-u25.jpg H H ND ND
3m H H graphic file with name c8ra01440j-u26.jpg 0.47 ± 0.04 0.290 ± 0.002
3n H H graphic file with name c8ra01440j-u27.jpg 0.95 ± 0.27 1.6 ± 0.1
3o H CH3 graphic file with name c8ra01440j-u28.jpg 5.60 ± 0.03 0.74 ± 0.04
a

The IC50 value was interpolated from dose–response data with six different concentrations. Each test was performed in duplicate. Data represent the average of duplicate measurements.

b

Not determined due to the lack of significant inhibition at the concentration of 10 μM.