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. Author manuscript; available in PMC: 2008 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2006 Oct 10;15(1):495–510. doi: 10.1016/j.bmc.2006.09.039

Table 4.

Differential Indices of Lavendamycins

graphic file with name nihms14804t4.jpg
Differential Indexa
Tumor Cell Linesb
No. R1 R2 R3 R4 K/1 H/1.2 N/4.2 3LL
19 CH3CO CO2CH2CH3 H H 7.5 0.8 0.7 0.1
20 CH3CO CO2CH(CH2)5 H H 1.7 1.0 1.0 0.7
21 CH3CO CO2C5H11-i CH3 H 0.9 1.1 1.2 0.6
22 CH3CO CO2CH2CH2N(CH3)2 H H 2.6 1.5 1.3 0.7
23 CH3CO CO2CH2CH2N(CH3)2 CH3 H 1.5 1.0 1.0 0.2
24 CH3CO CO2C4H9-n H OCH3 1.1 1.2 1.1 <0.7
25 CH3CO CO2C4H9-n H F 1.9 0.9 0.8 0.3
26 ClCH2CO CO2CH3 CH3 H 0.7 1.0 0.8 0.3
27 CH3CO CO2C4H9-n H OCH3 1.1 1.2 1.1 <0.7
28 ClCH2CO CO2C8H17-n H H >2.2 1.0 1.0 1.0
29 n-C3H7CO CO2CH3 H H 1.4 1.1 1.1 0.5
30 n-C3H7CO CO2CH3 CH3 H 1.0 0.8 0.8 0.4
31 n-C3H7CO CO2C5H11-i H H 1.6 2.7 1.5 0.4
32 n-C3H7CO CO2C8H17-n H H >10 2 >2.2 >2
33 i-C3H7CO CO2CH3 H H 1.4 1.1 1.1 0.5
34 i-C3H7CO CO2C4H9-n H H 2.3 1.5 1.8 1.0
35 H CO2CH3 CH3 H 3.2 0.9 1.6 0.4
36 CH3CO H H H 0.9 1.0 0.8 0.1
37 CH3CO CH2OH H H 1.2 1.2 1.1 0.6
38 CH3CO CO2H H H 2.1 1.4 1.5 0.4
39 CH3CO CONH2 H H 2.5 1.5 4.1 4.3
40 CH3CO CO2CH3 H H 4.5 1 1 0.6
41 CH3CO CO2C5H11-i H H 18 1.1 1.1 1.0
42 CH3CO CO2C8H17-n H H >132 4.3 3.6 1.0
43 CH3CO CO2CH2Ph H H 1.0 <0.9 <0.3 <0.3
44 CH3CO CO2CH3 CH3 H 9.0 1.3 N.T. 0.03
45 ClCH2CO CO2C5H11-i H H 2.4 1.0 1.1 0.4
46 n-C3H7CO CO2C4H9-n H H 1.3 1.6 0.9 0.3
a

Differential index of cytotoxicity was determined by dividing the LC50 value for the normal rat kidney epithelial cells ( NRK) by the LC50 value for the tumor cells. Index values for analogues which reflected LC50 activity at concentrations at least two times lower toward tumor cells than to normal cells are shown in bold.

b

See footnotes for Table 2.