TY  - JOUR
AU  - Palermo, Giulia
AU  - Minniti, Elirosa
AU  - Greco, Maria Laura
AU  - Riccardi, Laura
AU  - Simoni, Elena
AU  - Convertino, Marino
AU  - Marchetti, Chiara
AU  - Rosini, Michela
AU  - Sissi, Claudia
AU  - Minarini, Anna
AU  - De Vivo, Marco
TI  - An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512
JO  - Chemical communications
VL  - 51
IS  - 76
SN  - 1364-548X
CY  - Cambridge
PB  - Soc.
M1  - FZJ-2017-03092
SP  - 14310 - 14313
PY  - 2015
AB  - Combined computational–experimental analyses explain and quantify the spermine-vectorized F14512's boosted potency as a topoII poison. We found that an optimized polyamine moiety boosts drug binding to the topoII/DNA cleavage complex, rather than to the DNA alone. These results provide new structural bases and key reference data for designing new human topoII poisons.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000361073400005
C6  - pmid:26234198
DO  - DOI:10.1039/C5CC05065K
UR  - https://juser.fz-juelich.de/record/829379
ER  -