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. 2018 Feb 28;23(3):536. doi: 10.3390/molecules23030536

Table 2.

Novel 11β-HSD1 inhibitors featuring the 4-azapentacyclo[5.3.2.02,6.08,10]dodec-11-ene polycycle a,b.

graphic file with name molecules-23-00536-i002.jpg
Cp RHS hHSD1 % inh at 10 µM b hHSD1 IC50 (µM) HEK hHSD1 % inh at 10 µM c HEK hHSD2 % inh at 10 µM c HLM % Parent d
2 graphic file with name molecules-23-00536-i003.jpg 100 0.019 100 69 27
4 graphic file with name molecules-23-00536-i004.jpg 100 0.546 77 84 85
5 graphic file with name molecules-23-00536-i005.jpg 100 4.265 ND ND ND
6 graphic file with name molecules-23-00536-i006.jpg 100 0.666 41 71 60
7 graphic file with name molecules-23-00536-i007.jpg 49 ND ND ND ND
8 graphic file with name molecules-23-00536-i008.jpg 100 0.045 100 86 13
9 graphic file with name molecules-23-00536-i009.jpg 100 0.056 100 87 44
10 graphic file with name molecules-23-00536-i010.jpg 0 ND ND ND ND
11 graphic file with name molecules-23-00536-i011.jpg 23 ND ND ND ND
12 graphic file with name molecules-23-00536-i012.jpg 3 ND ND ND ND
13 graphic file with name molecules-23-00536-i013.jpg 0 ND ND ND ND
14 graphic file with name molecules-23-00536-i014.jpg 100 5.441 ND ND ND
15 graphic file with name molecules-23-00536-i015.jpg 100 11.560 ND ND ND
16 graphic file with name molecules-23-00536-i016.jpg 100 0.377 100 53 13

a See Experimental section for further details; b Percentage inhibition was determined relative to a no inhibitor control; c HEK293 cells stably transfected with the full-length gene coding for human either 11β-HSD1 or 11β-HSD2 were used; d Percentage of remaining compound after 30-min incubation period in HLM. ND, not determined.