. Author manuscript; available in PMC: 2014 Dec 6.

Published in final edited form as: J Org Chem. 2013 Nov 21;78(23):11970–11984. doi: 10.1021/jo4020112

Table 4.

48-hour activity of (−)-agelastatins A–F against human blood cancer cell lines.^a

Cmpd	CEM (μM)	Jurkat (μM)	Daudi (μM)	HL-60 (μM)	CA46 (μM)
(−)-1	0.020 ± 0.002	0.074 ± 0.007	0.020 ± 0.003	0.138 ± 0.066	0.187 ± 0.071
(−)-2	0.29 ± 0.20	0.75 ± 0.44	0.46 ± 0.28	2.4 ± 1.0	1.07 ± 0.42
(−)-3	2.1 ± 1.3	5.31 ± 0.35	7.2 ± 2.9	>10	>10
(−)-4	0.074 ± 0.025	0.210 ± 0.063	0.202 ± 0.015	0.54 ± 0.12	0.46 ± 0.24
(−)-5	0.83 ± 0.37	1.50 ± 0.33	1.41 ± 0.53	4.6 ± 3.6	2.45 ± 0.95
(−)-6	>10	>10	>10	>10	>10

Cell lines: CEM, acute lymphoblastic leukemia; Jurkat, acute T-cell leukemia; Daudi, Burkitt’s lymphoma; HL-60, acute promyelocytic leukemia; CA46, Burkitt’s lymphoma; 48-hour IC₅₀ values (in μM) as determined by MTS; MTS = 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium).