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. 2016 Feb;23(6):520–577. doi: 10.2174/0929867323666151223095839
Compound R5 R7 a/b Min. DNA un-winding conc.a
(μg/mL)
Decatanation inhib.b
(μg/mL)
A549c
CC50
(μg/mL)
P388d
CC50
(μg/mL)
P388/
ADRe
(MDR)
CC50 (μg/mL)
56j H B H/H 3 2 0.59 0.04 0.39
57 H C H/H 128 >100 2 0.5 *
58 H A H/Me * * 0.12 0.038 0.24
59 H A Me/Me * * 0.034 0.012 *
60 H A H/OMe * * 0.29 0.05 *
61 H A H/Ph * * 0.16 0.07 *
62 NH2 A H/H * * 0.069 0.0053 *
63 NH2 B H/H * * 0.10 0.0047 *
64 NHMe A H/H * * 0.39 0.039 *
65 NH2 D H/H * * 0.06 0.030 *
66 NHMe D H/H * * 1.1 0.79 *
67 NMe2 D H/H * * 6.4 3.9 *

a Measured at 10mM MgCl2; b drug concentration that inhibits 50% of the conversion of catenated to decatenated k-DNA catalyzed by calf thymus topoisomerase II; c human breast cancer cell line; d murine leukemia cell line; e adriamycin resistant/multidrug resistant; f doxorubicin (adriamycin); g 55 = A-62176 (racemate); h R-enantiomer of 55; i S-enantiomer of 55; j 56 = A-74932 (diasteromeric mixture); *data not reported.