11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents

Wei Feng; Mavurapu Satyanarayana; Yuan Chin Tsai; Angela A. Liu; Leroy F. Liu; Edmond J. LaVoie

doi:10.1016/j.bmc.2008.08.018

11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents

Wei Feng, Mavurapu Satyanarayana, Yuan Chin Tsai, Angela A. Liu, Leroy F. Liu, Edmond J. LaVoie

研究成果: 雜誌貢獻 › 文章 › 同行評審

11 引文斯高帕斯（Scopus）

摘要

Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.

原文	英語
頁（從 - 到）	8598-8606
頁數	9
期刊	Bioorganic and Medicinal Chemistry
卷	16
發行號	18
DOIs	https://doi.org/10.1016/j.bmc.2008.08.018
出版狀態	已發佈 - 9月 15 2008
對外發佈	是

ASJC Scopus subject areas

生物化學
分子醫學
分子生物學
藥學科學
藥物發現
臨床生物化學
有機化學

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10.1016/j.bmc.2008.08.018

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title = "11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents",

abstract = "Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.",

keywords = "Antitumor agents, Benzo[i]phenanthridines, Cytotoxicity, Multidrug resistance, Photocyclization, Topoisomerase I",

author = "Wei Feng and Mavurapu Satyanarayana and Tsai, {Yuan Chin} and Liu, {Angela A.} and Liu, {Leroy F.} and LaVoie, {Edmond J.}",

note = "Funding Information: This study was supported by the National Cancer Institute, Grants CA098127 (E.J.L.) and CA39662 (L.F.L.), and Genzyme Corporation.",

year = "2008",

month = sep,

day = "15",

doi = "10.1016/j.bmc.2008.08.018",

language = "English",

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T1 - 11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting 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 the National Cancer Institute, Grants CA098127 (E.J.L.) and CA39662 (L.F.L.), and Genzyme Corporation.

PY - 2008/9/15

Y1 - 2008/9/15

N2 - Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.

AB - Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.

KW - Antitumor agents

KW - Benzo[i]phenanthridines

KW - Cytotoxicity

KW - Multidrug resistance

KW - Photocyclization

KW - Topoisomerase I

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VL - 16

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JO - Bioorganic and Medicinal Chemistry

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ER -

11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents

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ASJC Scopus subject areas

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