Table 2

Pseudo first-order rate constants for decay of cleavable complexes stabilized by 7,10-disubstituted CPTs

Camptothecin AnalogRate Constant τ
From plasmid2-aFrom nuclei2-b
min−1
CPT0.061  ± 0.0100.130  ± 0.013
C1CPT0.066  ± 0.008
C2CPT0.034  ± 0.006
C3CPT0.024  ± 0.009
C4CPT0.050  ± 0.005
OHCPT0.082  ± 0.004
OHC1CPT0.108  ± 0.012
OHC2CPT0.061  ± 0.013
OHC3CPT0.064  ± 0.006
OHC4CPT0.058  ± 0.010
OMeCPT0.131  ± 0.017
OMeC1CPT0.054  ± 0.012
OMeC2CPT0.044  ± 0.006
OMeC3CPT0.054  ± 0.014
OMeC4CPT0.045  ± 0.024
MDCPT0.028  ± 0.0070.036  ± 0.011
MDC1CPT0.049  ± 0.008
MDC2CPT0.040  ± 0.0060.045  ± 0.019
MDC3CPT0.114  ± 0.012
MDC4CPT0.045  ± 0.009
CMMD (chloromethyl)0.277  ± 0.0480.088  ± 0.011
  • 2-a Disappearance of cleavable complexes with time after addition of 100-fold excess sheared salmon sperm DNA.

  • 2-b Disappearance of PDCs in CEM nuclei after suspension of nuclei in drug-free buffer.