Abstract
Substituted benzo[i]phenanthridines that have incorporated within their structure an 8,9-methylenedioxy group can exhibit topoisomerase I-targeting activity. Structure-activity studies were performed to examine the influence of saturation at the 11,12-positions of several substituted 8,9-methylenedioxybenzo[i]phenanthridines. The activities of these dihydro analogues were compared to those of their unsaturated analogues. In addition, the influence of varying substituents at the 2- and 3-positions within the A-ring of these 8,9-methylenedioxybenzo[i]phenanthridines on their relative potency as topoisomerase I-targeting agents and cell proliferation as determined using the MTT assay was investigated. 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and its 11,12-dihydro derivative were among the more potent analogues evaluated with regard to topoisomerase I-targeting activity and cytotoxicity.
| Original language | English |
|---|---|
| Pages (from-to) | 3795-3805 |
| Number of pages | 11 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 11 |
| Issue number | 17 |
| DOIs | |
| Publication status | Published - Aug 15 2003 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
8,9-Methylenedioxybenzo[i]phenanthridines : Topoisomerase I-targeting activity and cytotoxicity. / Li, Dajie; Zhao, Baoping; Sim, Sai Peng; Li, Tsai Kun; Liu, Angela; Liu, Leroy-Fong; LaVoie, Edmond J.
In: Bioorganic and Medicinal Chemistry, Vol. 11, No. 17, 15.08.2003, p. 3795-3805.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - 8,9-Methylenedioxybenzo[i]phenanthridines
T2 - Topoisomerase I-targeting activity and cytotoxicity
AU - Li, Dajie
AU - Zhao, Baoping
AU - Sim, Sai Peng
AU - Li, Tsai Kun
AU - Liu, Angela
AU - Liu, Leroy-Fong
AU - LaVoie, Edmond J.
PY - 2003/8/15
Y1 - 2003/8/15
N2 - Substituted benzo[i]phenanthridines that have incorporated within their structure an 8,9-methylenedioxy group can exhibit topoisomerase I-targeting activity. Structure-activity studies were performed to examine the influence of saturation at the 11,12-positions of several substituted 8,9-methylenedioxybenzo[i]phenanthridines. The activities of these dihydro analogues were compared to those of their unsaturated analogues. In addition, the influence of varying substituents at the 2- and 3-positions within the A-ring of these 8,9-methylenedioxybenzo[i]phenanthridines on their relative potency as topoisomerase I-targeting agents and cell proliferation as determined using the MTT assay was investigated. 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and its 11,12-dihydro derivative were among the more potent analogues evaluated with regard to topoisomerase I-targeting activity and cytotoxicity.
AB - Substituted benzo[i]phenanthridines that have incorporated within their structure an 8,9-methylenedioxy group can exhibit topoisomerase I-targeting activity. Structure-activity studies were performed to examine the influence of saturation at the 11,12-positions of several substituted 8,9-methylenedioxybenzo[i]phenanthridines. The activities of these dihydro analogues were compared to those of their unsaturated analogues. In addition, the influence of varying substituents at the 2- and 3-positions within the A-ring of these 8,9-methylenedioxybenzo[i]phenanthridines on their relative potency as topoisomerase I-targeting agents and cell proliferation as determined using the MTT assay was investigated. 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine and its 11,12-dihydro derivative were among the more potent analogues evaluated with regard to topoisomerase I-targeting activity and cytotoxicity.
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UR - http://www.scopus.com/inward/citedby.url?scp=0041620599&partnerID=8YFLogxK
U2 - 10.1016/S0968-0896(03)00394-8
DO - 10.1016/S0968-0896(03)00394-8
M3 - Article
C2 - 12901925
AN - SCOPUS:0041620599
VL - 11
SP - 3795
EP - 3805
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 17
ER -