Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: Design, synthesis and potential antitumor activity

Aibin Wu; Yufang Xu; Xuhong Qian

doi:10.1016/j.bmc.2008.11.080

Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: Design, synthesis and potential antitumor activity

Aibin Wu
, Yufang Xu
, Xuhong Qian^*

^*Corresponding author for this work

East China University of Science and Technology

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

61 Scopus citations

Abstract

A series of novel naphthalimide derivatives with flexible leucine side chains 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 moderate antitumor activities with the IC₅₀ values of 10^-6-10^-5 M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.

Original language	English
Pages (from-to)	592-599
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	2
DOIs	https://doi.org/10.1016/j.bmc.2008.11.080
State	Published - 15 Jan 2009
Externally published	Yes

Keywords

Antitumor
Leucine
MCF-7
Naphthalimide

UN SDGs

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

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10.1016/j.bmc.2008.11.080

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title = "Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: Design, synthesis and potential antitumor activity",

abstract = "A series of novel naphthalimide derivatives with flexible leucine side chains 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 moderate antitumor activities with the IC50 values of 10-6-10-5 M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.",

keywords = "Antitumor, Leucine, MCF-7, Naphthalimide",

author = "Aibin Wu and Yufang Xu and Xuhong Qian",

year = "2009",

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doi = "10.1016/j.bmc.2008.11.080",

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TY - JOUR

T1 - Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain

T2 - Design, synthesis and potential antitumor activity

AU - Wu, Aibin

AU - Xu, Yufang

AU - Qian, Xuhong

PY - 2009/1/15

Y1 - 2009/1/15

N2 - A series of novel naphthalimide derivatives with flexible leucine side chains 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 moderate antitumor activities with the IC50 values of 10-6-10-5 M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.

AB - A series of novel naphthalimide derivatives with flexible leucine side chains 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 moderate antitumor activities with the IC50 values of 10-6-10-5 M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.

KW - Antitumor

KW - Leucine

KW - MCF-7

KW - Naphthalimide

UR - https://www.scopus.com/pages/publications/58549117087

U2 - 10.1016/j.bmc.2008.11.080

DO - 10.1016/j.bmc.2008.11.080

M3 - 文章

C2 - 19109022

AN - SCOPUS:58549117087

SN - 0968-0896

VL - 17

SP - 592

EP - 599

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 2

ER -

Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: Design, synthesis and potential antitumor activity

Abstract

Keywords

UN SDGs

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