Table 1.

TG2 inhibitory activity of enantiopure azido- and alkynyl-DHI compounds. Compounds 17 and 18 have a stereochemically altered DHI moiety, and are therefore considerably less potent than their diastereomeric analogs, 11 and 12, respectively.

Cmpd	K I(μM)	kinh (min−1)	kinh/KI(mM−1 min−1)	Cmpd	K I(μM)	kinh (min−1)	kinh/KI(mM−1 min−1)
3	280	1.63	5.8	11	7.0	0.13	19
4	15	0.23	15	12	1.8	0.052	30
5	100	0.82	8.0	13	41	0.51	12
6	19	0.31	16	14	47	0.53	11
7	9.2	0.12	13	15	22	0.13	6.1
8	4.2	0.016	4.0	16	19	0.73	38
9	13	0.15	11	17	51	0.21	4.2
10	12	0.14	8.0	18	38	0.27	7.2