Table 2.

Extended C7-pyrazole modifications

Compd	R	Aurora-A IC50 (μM)	Aurora-B IC50 (μM)	MLM/HLM% met/30 min
14a		0.036	0.296	72/72
14b		0.046	0.235	97/87
14c		0.126	0.354	98/82
14d		0.035	0.075	35/37
14e		0.014	0.017	97/95
14f		0.017	0.031	100/92
14g		0.018	0.032	53/38

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