Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation

Aibin Wu; Yufang Xu; Xuhong Qian; Jin Wang; Jianwen Liu

doi:10.1016/j.ejmech.2009.07.011

Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation

Aibin Wu
, Yufang Xu
, Xuhong Qian^*
, Jin Wang
, Jianwen Liu

^*Corresponding author for this work

East China University of Science and Technology

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

40 Scopus citations

Abstract

A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had comparable antitumor activities over Amonafide with the IC₅₀ values of 10^-6 to 10^-5 M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G₂/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.

Original language	English
Pages (from-to)	4674-4680
Number of pages	7
Journal	European Journal of Medicinal Chemistry
Volume	44
Issue number	11
DOIs	https://doi.org/10.1016/j.ejmech.2009.07.011
State	Published - Nov 2009
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antitumor
Apoptosis
Cytotoxicity
G/M arrest
Naphthalimide

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10.1016/j.ejmech.2009.07.011

Cite this

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title = "Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation",

abstract = "A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had comparable antitumor activities over Amonafide with the IC50 values of 10-6 to 10-5 M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G2/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.",

keywords = "Antitumor, Apoptosis, Cytotoxicity, G/M arrest, Naphthalimide",

author = "Aibin Wu and Yufang Xu and Xuhong Qian and Jin Wang and Jianwen Liu",

year = "2009",

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doi = "10.1016/j.ejmech.2009.07.011",

language = "英语",

volume = "44",

pages = "4674--4680",

journal = "European Journal of Medicinal Chemistry",

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publisher = "Elsevier Masson s.r.l.",

number = "11",

}

TY - JOUR

T1 - Novel naphthalimide derivatives as potential apoptosis-inducing agents

T2 - Design, synthesis and biological evaluation

AU - Wu, Aibin

AU - Xu, Yufang

AU - Qian, Xuhong

AU - Wang, Jin

AU - Liu, Jianwen

PY - 2009/11

Y1 - 2009/11

N2 - A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had comparable antitumor activities over Amonafide with the IC50 values of 10-6 to 10-5 M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G2/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.

AB - A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had comparable antitumor activities over Amonafide with the IC50 values of 10-6 to 10-5 M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G2/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.

KW - Antitumor

KW - Apoptosis

KW - Cytotoxicity

KW - G/M arrest

KW - Naphthalimide

UR - https://www.scopus.com/pages/publications/70349772961

U2 - 10.1016/j.ejmech.2009.07.011

DO - 10.1016/j.ejmech.2009.07.011

M3 - 文章

C2 - 19643513

AN - SCOPUS:70349772961

SN - 0223-5234

VL - 44

SP - 4674

EP - 4680

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11

ER -

Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation

Abstract

UN SDGs

Keywords

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