TY - JOUR
T1 - 12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents
AU - Feng, Wei
AU - Satyanarayana, Mavurapu
AU - Tsai, Yuan Chin
AU - Liu, Angela A.
AU - Liu, Leroy F.
AU - LaVoie, Edmond J.
N1 - Funding Information:
This study was supported by Grant CA098127 (E.J.L), Grant CA39662 (L.F.L.) and Grant CA077433 (L.F.L.) from the National Cancer Institute and support from the Genzyme Corporation.
PY - 2009/4/1
Y1 - 2009/4/1
N2 - 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and a few of its 12-substituted analogs are active as TOP1-targeting agents. Studies were performed to further evaluate the potential of this series of non-camptothecin TOP1-targeting agents. The influence of a hydroxymethyl, formyl, N,N-dimethylaminomethyl, 2-(N,N-dimethylamino)ethyl, 3-(N,N-dimethylamino)propyl), and 4-(N,N-dimethylamino)butyl substituent at the 12-position on TOP1-targeting activity and tumor cell growth was evaluated. In addition, the relative pharmacologic activities of the 12-carboxamide analog, as well as its N-methyl and N,N-dimethyl derivatives were assessed.
AB - 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and a few of its 12-substituted analogs are active as TOP1-targeting agents. Studies were performed to further evaluate the potential of this series of non-camptothecin TOP1-targeting agents. The influence of a hydroxymethyl, formyl, N,N-dimethylaminomethyl, 2-(N,N-dimethylamino)ethyl, 3-(N,N-dimethylamino)propyl), and 4-(N,N-dimethylamino)butyl substituent at the 12-position on TOP1-targeting activity and tumor cell growth was evaluated. In addition, the relative pharmacologic activities of the 12-carboxamide analog, as well as its N-methyl and N,N-dimethyl derivatives were assessed.
KW - Benzo[i]phenanthridines
KW - Cytotoxicity
KW - Structure-activity
KW - Topoisomerase I
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U2 - 10.1016/j.bmc.2009.02.023
DO - 10.1016/j.bmc.2009.02.023
M3 - Article
C2 - 19303306
AN - SCOPUS:62949117616
SN - 0968-0896
VL - 17
SP - 2877
EP - 2885
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 7
ER -