. Author manuscript; available in PMC: 2013 Aug 9.

Published in final edited form as: J Med Chem. 2012 Jul 23;55(15):6751–6761. doi: 10.1021/jm3001218

Table 3.

Antiproliferative activity of new E-ring dihydroxylated analogs of R-cryptopleurine

Cmpd	E-ring oxygenation	IC₅₀ (nM)				Predicted C.brain/C.blood
Cmpd	E-ring oxygenation	A549	DU145	KB	KBvin	Predicted C.brain/C.blood
24a	12S,13S-OH	550 ± 67	600 ± 93	840 ± 120	2170 ± 350	0.068
24b	12R,13R-OH	14480 ± 1540	1709 ± 260	17520 ± 1660	12560 ± 1350	0.068
R-cryptopleurine	--	1.38 ± 0.56	1.59 ± 0.53	1.51 ± 0.33	1.91 ± 0.63 (HCT-8)	0.281