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. 2015 Oct 1;25(19):4203–4209. doi: 10.1016/j.bmcl.2015.08.003

Table 1.

C7-Pyrazole modifications

graphic file with name fx2.jpg

Compd R Aurora-A IC50 (μM) Aurora-B IC50 (μM) MLM/HLM% met/30 min
7a graphic file with name fx3.gif 0.212 ± 0.107 0.461 ± 0.147 40/43
7b graphic file with name fx4.gif 0.182 0.347 52/39
7c graphic file with name fx5.gif 0.322 0.458 31/28
7d graphic file with name fx6.gif 0.190 0.271 37/16
7e graphic file with name fx7.gif >10 >10 31/20

IC50s are mean values of two independent determinations or mean (±SD) for n > 2.17

MLM/HLM: percentage of compound metabolised after a 30 min incubation.18