Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

Zhigang Li; Qing Yang; Xuhong Qian

doi:10.1016/j.bmcl.2005.04.012

Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

Zhigang Li
, Qing Yang
, Xuhong Qian^*

^*此作品的通讯作者

Dalian University of Technology
East China University of Science and Technology

科研成果: 期刊稿件 › 文章 › 同行评审

36 引用（Scopus）

摘要

A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A₁ showed both efficient antitumor activities against cell lines of A549 and P388 with IC₅₀ of 82.8 and 31 nM, respectively. A₃ was the strongest antitumor agent against A549 with the IC₅₀ of 20.8 nM. A₂, the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.

源语言	英语
页（从-至）	3143-3146
页数	4
期刊	Bioorganic and Medicinal Chemistry Letters
卷	15
期	12
DOI	https://doi.org/10.1016/j.bmcl.2005.04.012
出版状态	已出版 - 15 6月 2005
已对外发布	是

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title = "Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains",

abstract = "A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A1 showed both efficient antitumor activities against cell lines of A549 and P388 with IC50 of 82.8 and 31 nM, respectively. A3 was the strongest antitumor agent against A549 with the IC50 of 20.8 nM. A2, the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.",

keywords = "Antitumor, Intercalate, Methylthiazonaphthalimide, Photocleaver",

author = "Zhigang Li and Qing Yang and Xuhong Qian",

year = "2005",

month = jun,

day = "15",

doi = "10.1016/j.bmcl.2005.04.012",

language = "英语",

volume = "15",

pages = "3143--3146",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

AU - Li, Zhigang

AU - Yang, Qing

AU - Qian, Xuhong

PY - 2005/6/15

Y1 - 2005/6/15

N2 - A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A1 showed both efficient antitumor activities against cell lines of A549 and P388 with IC50 of 82.8 and 31 nM, respectively. A3 was the strongest antitumor agent against A549 with the IC50 of 20.8 nM. A2, the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.

AB - A series of methylthiazonaphthalimides was synthesized and quantitatively evaluated as efficient DNA intercalators, antitumor agents and DNA photocleavers. A1 showed both efficient antitumor activities against cell lines of A549 and P388 with IC50 of 82.8 and 31 nM, respectively. A3 was the strongest antitumor agent against A549 with the IC50 of 20.8 nM. A2, the most efficient DNA intercalator, was found to be the strongest DNA photocleaver via superoxide anion. An explanation was given for the disaccord between antitumor and DNA photocleaving activities.

KW - Antitumor

KW - Intercalate

KW - Methylthiazonaphthalimide

KW - Photocleaver

UR - https://www.scopus.com/pages/publications/19944413311

U2 - 10.1016/j.bmcl.2005.04.012

DO - 10.1016/j.bmcl.2005.04.012

M3 - 文章

C2 - 15876532

AN - SCOPUS:19944413311

SN - 0960-894X

VL - 15

SP - 3143

EP - 3146

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains

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