Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 2877-2885 |
| Number of pages | 9 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 17 |
| Issue number | 7 |
| DOIs | |
| Publication status | Published - Apr 1 2009 |
| Externally published | Yes |
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Keywords
- Benzo[i]phenanthridines
- Cytotoxicity
- Structure-activity
- Topoisomerase I
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry
- Molecular Medicine
- Molecular Biology
- Clinical Biochemistry
- Biochemistry
Cite this
12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. / Feng, Wei; Satyanarayana, Mavurapu; Tsai, Yuan Chin; Liu, Angela A.; Liu, Leroy F.; LaVoie, Edmond J.
In: Bioorganic and Medicinal Chemistry, Vol. 17, No. 7, 01.04.2009, p. 2877-2885.Research output: Contribution to journal › Article
}
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.
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
UR - http://www.scopus.com/inward/record.url?scp=62949117616&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=62949117616&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2009.02.023
DO - 10.1016/j.bmc.2009.02.023
M3 - Article
VL - 17
SP - 2877
EP - 2885
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 7
ER -