Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: Synthesis and biological evaluation

Hong Yin; Yufang Xu; Xuhong Qian; Yuanli Li; Jianwen Liu

doi:10.1016/j.bmcl.2007.02.015

Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: Synthesis and biological evaluation

Hong Yin
, Yufang Xu^*
, Xuhong Qian
, Yuanli Li
, Jianwen Liu

^*Corresponding author for this work

East China University of Science and Technology

Research output: Contribution to journal › Article › peer-review

23 Scopus citations

Abstract

Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.

Original language	English
Pages (from-to)	2166-2170
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2007.02.015
State	Published - 15 Apr 2007
Externally published	Yes

Keywords

Biological evaluation
Hypoxic solid tumor
N-Oxide of naphthalimides
Prodrug leads
Synthesis

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10.1016/j.bmcl.2007.02.015

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abstract = "Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.",

keywords = "Biological evaluation, Hypoxic solid tumor, N-Oxide of naphthalimides, Prodrug leads, Synthesis",

author = "Hong Yin and Yufang Xu and Xuhong Qian and Yuanli Li and Jianwen Liu",

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T2 - Synthesis and biological evaluation

AU - Yin, Hong

AU - Xu, Yufang

AU - Qian, Xuhong

AU - Li, Yuanli

AU - Liu, Jianwen

PY - 2007/4/15

Y1 - 2007/4/15

N2 - Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.

AB - Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.

KW - Biological evaluation

KW - Hypoxic solid tumor

KW - N-Oxide of naphthalimides

KW - Prodrug leads

KW - Synthesis

UR - https://www.scopus.com/pages/publications/33947595807

U2 - 10.1016/j.bmcl.2007.02.015

DO - 10.1016/j.bmcl.2007.02.015

M3 - 文章

C2 - 17331719

AN - SCOPUS:33947595807

SN - 0960-894X

VL - 17

SP - 2166

EP - 2170

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: Synthesis and biological evaluation

Abstract

Keywords

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