TY - JOUR
T1 - Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity
AU - Ruchelman, Alexander L.
AU - Zhu, Shejin
AU - Zhou, Nai
AU - Liu, Angela
AU - Liu, Leroy F.
AU - LaVoie, Edmond J.
N1 - Funding Information:
This study was supported by Grant CA098127 (E.J.L.) and Grant CA39662 (L.F.L.) and Grant CA077433 (L.F.L.) from the National Cancer Institute.
PY - 2004/11/15
Y1 - 2004/11/15
N2 - The exceptional TOP1-targeting activity and antitumor activity of ARC-111, 1, prompted studies on similarly substituted benzo[i]phenanthridine-12- carboxylic ester and amide derivatives. These studies were extended to include 6-substituted 8,9-dimethoxy-2,3-methylenedioxy-dibenzo[c,h][2,6]naphthyridin-5- ones, which represent reversed lactam analogues of 1. Several of these analogues retained the potent TOP1-targeting activity and cytotoxicity observed for ARC-111.
AB - The exceptional TOP1-targeting activity and antitumor activity of ARC-111, 1, prompted studies on similarly substituted benzo[i]phenanthridine-12- carboxylic ester and amide derivatives. These studies were extended to include 6-substituted 8,9-dimethoxy-2,3-methylenedioxy-dibenzo[c,h][2,6]naphthyridin-5- ones, which represent reversed lactam analogues of 1. Several of these analogues retained the potent TOP1-targeting activity and cytotoxicity observed for ARC-111.
KW - Anticancer
KW - Benzo[i]phenanthridines
KW - Cytotoxic agents
KW - Dibenzo[c,h]naphthyridines
KW - Topoisomerase I
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U2 - 10.1016/j.bmcl.2004.08.070
DO - 10.1016/j.bmcl.2004.08.070
M3 - Article
C2 - 15482929
AN - SCOPUS:5144223304
SN - 0960-894X
VL - 14
SP - 5585
EP - 5589
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 22
ER -