BND-12, a novel nonhaematotoxic naphthalimide derivative, inhibits tumour growth and metastasis of hepatocellular carcinoma

Xie, Songqiang; Li, Qian; Zhang, Yahong; Li, Zhan; Zhao, Jin; Wang, Chaojie

doi:10.1111/j.2042-7158.2012.01519.x

Cited by 2 publications

(2 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Cell migration and invasion are the most prominent features of malignant cell behavior. Many reports [ 38 , 39 ] showed that naphthalimide derivatives could inhibit tumor cells migration and invasion in vivo. In this study, compound 3a inhibited migration and invasion of SMMC-7721 and HepG2 cells using scratch assay and transwell invasion assay in vitro.…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma

Chang

Zhao

et al. 2017

Molecules

View full text Add to dashboard Cite

Two kinds of naphthalimide derivatives were synthesized and evaluated for in vitro their anti-hepatocellular carcinoma properties. Compound 3a with a fused thiazole fragment to naphthalimide skeleton inhibited cell migration of SMMC-7721 and HepG2, and further in vivo trials with two animal models confirmed that compound 3a moderately inhibited primary H22 tumor growth (52.6%) and potently interrupted lung metastasis (75.7%) without obvious systemic toxicity at the therapeutic dose. Mechanistic research revealed that compound 3a inhibited cancerous liver cell growth mostly by inducing G2/M phase arrest. Western blotting experiments corroborated that 3a could up-regulate the cell cycle related protein expression of cyclin B1, CDK1 and p21, and inhibit cell migration by elevating the E-cadherin and attenuating integrin α6 expression. Our study showed that compound 3a is a valuable lead compound worthy of further investigation.

show abstract

Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma

Chang

Zhao

et al. 2017

Molecules

View full text Add to dashboard Cite

show abstract

“…Naphthalimides have been reported to serve as core scaffold for many antitumor, anti‐inflammatory, antidepressant, antiprotozoal, and antiviral agents, and some of which were found without obvious systemic toxicities at the therapeutic dose (Kamal, Bolla, Srikanth, & Srivastava, 2013; Xie et al, 2012). Therefore, in the current study, we rationally designed and developed a series of naphthalimide compounds, which combine Aβ aggregation inhibition, neutralization of oxidative stress and neuroprotection, as MTDLs against AD.…”

Section: Introductionmentioning

confidence: 99%

Discovery and Characterization of Novel Naphthalimide Analogs as Potent Multitargeted Directed Ligands against Alzheimer's Disease

Gao

Chapman

2020

Drug Development Research

View full text Add to dashboard Cite

Current therapeutic drugs for Alzheimer's disease (AD) can only offer limited symptomatic benefits and do not halt disease progression. Multitargeted directed ligands (MTDLs) have been considered to be a feasible way to treat AD due to the multiple neuropathological processes in AD. Previous studies proposed that compounds containing two aromatic groups connected by a carbon chain should act as effective amyloid β (Aβ) aggregation inhibitors although the optimal length of the carbon chain has not been explored. In the current study, a series of naphthalimide analogs were designed and synthesized based on the proposed structure and multiple bioactivities beneficial to the AD treatment were reported. In vitro studies showed that compound 8, which has two aromatic groups connected by a two‐carbon chain, exhibited significant inhibition of Aβ aggregation through the prevention of elongation and association of Aβ fibril growth. Furthermore, this compound also displayed antioxidative activities and neuroprotection from Aβ monomer induced toxicity in primary cortical neurons. The results of the present study highlight a novel naphthalimide‐based compound 8 as a promising MTDL against AD. Its structural elements can be further explored for enhanced therapeutic capabilities.

show abstract

BND-12, a novel nonhaematotoxic naphthalimide derivative, inhibits tumour growth and metastasis of hepatocellular carcinoma

Abstract: BND-12 exerted potent effects against HCC in vivo and in vitro, importantly, it had no obvious systemic toxicity at the therapeutic dose.

Cited by 2 publications

References 19 publications

Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma

Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma

Discovery and Characterization of Novel Naphthalimide Analogs as Potent Multitargeted Directed Ligands against Alzheimer's Disease

Contact Info

Product

Resources

About