Table 5.

Cytotoxicity of aaptamine (1), isoaaptamine (2) and selected derivatives (5-12,14-18,20-28,30) against leukemia, solid tumor and normal cells in the disk diffusion soft-agar colony formation assay. Activities in bold print represent selectivity. Zones of growth inhibition are displayed in zone units from the disk edge in which 6.5 mm is arbitrarily designated as 200 zone units. Zones greater than 750 units are retested at 4-fold dilutions

		Mouse			Human
Cpd.	Dilution Factor	Leukemia L1210	Colon 38	Normal CFU-GM	Colon H-116	Lung H-125 M	Leukemia CEM
1	1/4	600	500	850	550	500	600
2	1	500	150	450	500	500	500
5	1	450	450	350	450	400	500
6	1	450	400	350	550	400	450
7	1	500	600	400	400	400	600
8	1	450	450	350	300	200	500
9	1	600	600	500	300	350	500
10	1	300	350	300	50	100	–
11	1/4	200	>1000	350	150	100	–
	1/16	100	450	150	–	–	–
12	1	600	650	500	200	250	–
14	1/4	300	550	800	150	200	–
	1/4	200	700	150	–	–	–
15	1/4	500	800	550	200	250	–
	1/16	200	700	350	–	–	–
16	1/4	600	>1000	550	400	400	500
	1/16	300	800	450	–	–	–
	1/64	200	600	400	–	–	–
17	1/4	700	>1000	800	400	500	500
	1/16	400	800	450	–	–	–
	1/64	150	750	350	–	–	–
18	1	650	600	500	400	400	400
20	1	450	550	450	350	400	400
21	1	450	350	600	300	250	350
22	1	350	350	250	150	150	–
23	1/4	300	400	400	400	250	300
24	1/4	350	200	350	350	250	500
25	1/4	500	200	–	400	350	500
26	1/4	450	400	400	400	300	400
27	1	600	600	550	400	350	300
28	1	600	600	500	500	500	600
30	1	300	300	350	250	200	–