Table 1.

Antiproliferative activity of β-Carbolines on human colon and pancreatic cancer cell lines.

Compound No.	R1	R2	R3	R4	R5	R6	R7	X	HCT116 (CCa) IC50 (µM)	HPAC (PCb) IC50 (µM)	Mia- PaCa2 (PCb) IC50 (µM)	Panc-1 (PCb) IC50 (µM)
1		H	H	H	H	OCH3	H	NH	7.0	NDc	ND	ND
2		H	H	H	OCH3	H	H	NH	0.51	0.56	0.49	0.58
3		H	H	H	H	OCH3	H	NH	ND	34.77	49.17	>50.00
4		H	H	H	OCH3	H	H	NH	26.10	>50.00	>50.00	>50.00
5		H	H	H	H	OCH3	H	NH	49.60	>50.00	>50.00	>50.00
6		H	H	H	OCH3	H	H	NH	>50.00	45.11	38.28	>50.00
7		H	H	H	OCH3	H	H	NH	5.70	7.37	4.70	10.46
8		H	H	H	H	OCH3	H	NH	33.50	44.88	36.73	>50.00
9		H	H	H	OCH3	H	H	NH	14.10	21.88	17.02	28.96
10		H	H	H	H	OCH3	H	NH	13.10	14.45	16.72	37.21
11		H	H	H	OCH3	H	H	NH	0.13	0.29	0.20	0.29
12		H	H	H	H	OCH3	H	NH	3.60	25.54	6.61	>50.00
13		H	H	H	OCH3	H	H	NH	0.90	5.83	2.58	7.52
14		H	H	H	H	OCH3	H	NH	12.80	>50.00	28.55	>50.00
15		H	H	H	OCH3	H	H	NH	9.00	15.92	9.81	21.20
16		H	H	H	H	OCH3	H	NH	15.10	34.40	24.06	>50.00
17		H	H	H	OCH3	H	H	NH	0.67	5.57	1.36	8.40
18		H	H	H	H	OCH3	H	NH	17.10	20.76	21.68	48.03
19		H	H	H	OCH3	H	H	NH	2.10	6.08	2.43	10.49
20		H	H	H	H	OCH3	H	NH	1.70	5.47	3.59	14.94
21		H	H	H	OCH3	H	H	NH	0.53	0.54	0.84	17.97
22		H	H	H	H	OCH3	H	NH	0.87	5.67	1.57	>50.00
23		H	H	H	OCH3	H	H	NH	33.50	44.79	37.05	>50.00
24		H	H	H	H	OCH3	H	NH	31.40	34.27	34.30	>50.00
25		H	H	H	OCH3	H	H	NH	1.80	9.38	2.23	19.76
26		H	H	H	H	OCH3	H	NH	2.43	17.63	20.74	33.28
27		H	H	H	OCH3	H	H	NH	2.22	23.12	47.19	>50.00
28		H	H	H		H	H	NH	ND	0.83	0.51	0.57
29		H	H	H	H	H	CH3	NH	2.60	6.39	3.54	>50.00
30		H	H	H	OCH3	H	H	NH	3.00	17.03	48.40	47.35
31		H	H	H	H	H	OCH3	NH	ND	20.54	31.90	26.49
32		H	H	H	OH	H	H	NH	ND	ND	ND	ND
33		H	Ph	H	OCH3	H	H	NH	ND	7.72	3.63	>10
34		H	H	H		H	H	NH	ND	3.83	0.58	6.11
35		H	H	CH3	H	H	H	NH	ND	4.03	1.17	4.56
36		H	H	H	OCH3	H	H	NH	ND	2.37	0.33	2.56
37		H	H	H	OCH3	H	H	NH	ND	6.18	1.17	2.92
38		H	H	H	CH3	H	H	NH	ND	>50.00	41.67	>50.00
39		H	H	H	OCH3	H	H	NH	ND	4.79	2.95	>50.00
40		H	H	H	Cl	H	H	S	ND	49.97	13.50	>50.00
41		H	H	H	H	H	H	O	ND	>50.00	33.59	>50.00
42		H	H	H	H	H	H	S	ND	>50	>50	>50
43		H	H	H	H	H	H	NH	ND	2.470	1.70	9.83
44		H	H	H	CH3	H	H	NH	ND	>50	13.08	>50
45		H	H	H	OCF3	H	H	NH	ND	35.48	8.63	>50
46		H	H	H	CN	H	H	NH	ND	>50.00	40.41	>50
47		CO2Et	H	H	OCH3	H	H	NH	ND	12.86	17.52	23.28
48		H	H	H	H	H	H	NCH3	ND	21.23	37.35	33.86
49		H	H	H	OCH3	H	H	NCH3	ND	44.19	34.02	41.27

^aCC = Colon cancer;

^bPC = Pancreatic cancer;

^cND = Not determined