Table 2.

Inhibitory effects of DOX, 2-pyrrolino-DOX (AN-201), and their conjugates with BN-like peptide carriers on the growth of CFPAC-1 human pancreatic cancer cell line and on DMS-53 human lung cancer cell line in vitro

Compound	Cell line	T/C Value
		3 × 10−11 M	10−10 M	3 × 10−10 M	10−9 M	3 × 10−8 M	10−7 M	3 × 10−7 M
Analogs with DOX
AN-253	CFPAC-1					79 (32)	18 (−7)	6 (−7)
	DMS-53					67 (−12)	33 (−15)	6 (−15)
AN-246	CFPAC-1					89	28	6
	DMS-53					70	23	2
AN-161	CFPAC-1					95	35	10
	DMS-53					80	39	5
AN-160	CFPAC-1					85	22	0
	DMS-53					68	24	0
AN-251	CFPAC-1					88	26	−2
	DMS-53					60	3	−12
DOX	CFPAC-1					68	22	4
	DMS-53					78	27	1
Analogs with AN-201
AN-254	CFPAC-1		95	13	−7
	DMS-53	45	−6	−15
AN-247	CFPAC-1		90	27	−7
	DMS-53	61	4	−14
AN-257	CFPAC-1		85	16	−7
	DMS-53	58	0	−18
AN-215	CFPAC-1		97	42	−7
	DMS-53	52	2	−15
AN-252	CFPAC-1		91	56	−6
	DMS-53	72	13	−19
AN-201	CFPAC-1		76	8	−5
	DMS-53	34	−7	−19

CFPAC-1 cells were incubated in Iscove’s modified Dulbecco’s medium with 10% fetal bovine serum (FBS) for 120 hr and DMS-53 cells were incubated for 140 hr in Waymouth’s MB 752/1 medium containing 10% FBS in 96-well plates. Relative cell number in treated and control plates was determined by crystal violet staining and expressed as T/C values where T/C = (T − C₀)/(C − C₀) × 100. [T = absorbance of treated cultures, C = absorbance of control cultures, C₀ = absorbance of cultures at the start of incubation (t = 0). Measured absorbance is proportionate to cell number.] Negative T/C values indicate a cell number smaller than the number originally seeded at t = 0—i.e., a cytocidal effect. The structures of the compounds are shown in Table 1. The carrier peptides had no effect on cell proliferation at 10⁻⁷ M and lower concentrations. T/C values in brackets are derived from results with a sample of AN-253 containing decomposition products.