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

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

36 Scopus citations

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.

Original language	English
Pages (from-to)	3143-3146
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2005.04.012
State	Published - 15 Jun 2005
Externally published	Yes

Keywords

Antitumor
Intercalate
Methylthiazonaphthalimide
Photocleaver

Access to Document

10.1016/j.bmcl.2005.04.012

Cite this

@article{c023d1b939a34de0824db6eda207fd75,

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",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "12",

}

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

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this