The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: Synthesis, cytotoxicity, DNA intercalation and photocleavage

Xiaolian Li; Yanjie Lin; Qianqian Wang; Yukun Yuan; Hua Zhang; Xuhong Qian

doi:10.1016/j.ejmech.2011.01.050

The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: Synthesis, cytotoxicity, DNA intercalation and photocleavage

Xiaolian Li, Yanjie Lin, Qianqian Wang, Yukun Yuan, Hua Zhang, Xuhong Qian

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

105 Scopus citations

Abstract

A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a, 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a, with an IC₅₀ could amount to 10^-7 M. The UV-vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III.

Original language	English
Pages (from-to)	1274-1279
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	46
Issue number	4
DOIs	https://doi.org/10.1016/j.ejmech.2011.01.050
State	Published - Apr 2011
Externally published	Yes

Keywords

Anticancer
Intercalation
Naphthalimides
Triazole

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10.1016/j.ejmech.2011.01.050

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author = "Xiaolian Li and Yanjie Lin and Qianqian Wang and Yukun Yuan and Hua Zhang and Xuhong Qian",

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doi = "10.1016/j.ejmech.2011.01.050",

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T1 - The novel anti-tumor agents of 4-triazol-1,8-naphthalimides

T2 - Synthesis, cytotoxicity, DNA intercalation and photocleavage

AU - Li, Xiaolian

AU - Lin, Yanjie

AU - Wang, Qianqian

AU - Yuan, Yukun

AU - Zhang, Hua

AU - Qian, Xuhong

PY - 2011/4

Y1 - 2011/4

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AB - A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a, 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a, with an IC50 could amount to 10-7 M. The UV-vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III.

KW - Anticancer

KW - Intercalation

KW - Naphthalimides

KW - Triazole

UR - https://www.scopus.com/pages/publications/79952281685

U2 - 10.1016/j.ejmech.2011.01.050

DO - 10.1016/j.ejmech.2011.01.050

M3 - 文章

C2 - 21345546

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SN - 0223-5234

VL - 46

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

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ER -

The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: Synthesis, cytotoxicity, DNA intercalation and photocleavage

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Keywords

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