Table 2. Antileukemic Activity of Select Natural and Synthetic Agelastatins against Various CLL Patient-Derived Cell Lines.

			in vitro cytotoxicity EC50 (μM)b
cmpd	Xa	Y	CLL3c	CLL4c	CLL5c	CLL6c
1a	Br	H	0.24	0.37	0.29	1.15
1d	Cl	H	3.80	1.98	0.34	2.20
1e	Cl	Cl	0.98	4.42	2.02	7.50
1g	I	H	6.61	3.04	3.06	12.9
1j	CF3	H	3.04	0.33	28.4	0.65
1n	CN	H	8.37	8.41	4.79	0.84
Flud			0.35	0.64	0.16	1.60

^aSee Figure 2 for the substituent key.

^bStandard error is ±0.01 μM for all data points.

^cCLL3–CLL6 = CLL patient cell lines.

^dFlu = fludarabine; see Figure 1 for the chemical structure.