Preclinical evaluation of a fluorinated bifendate derivative in triple-negative breast cancer: integrated in vitro and in vivo evidence of antitumor activity.

Lisa Zongyong Lin, Hai-Yi Huang, Yuanyuan Peng, Guo-Qiang Lin, Jinbo Hu, Ying Jiang

Abstract read

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Article in BMC cancer, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 · Who and what money

Authors and funding

6 authors.

Lisa Zongyong Lin *Department of General Surgery, Zhongshan Hospital, Fudan University, Shanghai, China.

Hai-Yi Huang *Department of General Surgery, Zhongshan Hospital, Fudan University, Shanghai, China.

Yuanyuan PengState Key Laboratory of Fluorine and Nitrogen Chemistry and Advanced Materials, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.

Guo-Qiang LinState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.

Jinbo HuState Key Laboratory of Fluorine and Nitrogen Chemistry and Advanced Materials, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China. jinbohu@sioc.ac.cn.

Ying JiangDepartment of General Surgery, Zhongshan Hospital, Fudan University, Shanghai, China. jiang.ying3@zs-hospital.sh.cn.

Funding

Fujian Provincial Natural Science Foundation of China 2022J011416

6 · The paper itself

Abstract

backgroundTriple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer with limited therapeutic options and poor clinical outcomes. Bifendate (DDB), a clinically used hepatoprotective agent, has shown modest antitumor activity. This study evaluated the antitumor activity of a fluorinated bifendate derivative (F-α-DDB-derivative) in TNBC models.

methodsMDA-MB-468 cells were treated with DDB or F-α-DDB-derivative to assess cell viability, migration, apoptosis, and Ki-67 expression. Antitumor efficacy and preliminary safety were further evaluated in a nude mouse xenograft model.

resultsF-α-DDB-derivative reduced cell viability in a concentration-dependent manner and showed greater potency than DDB, with a 24 h IC₅₀ of 25.06 µg/mL versus 105.00 µg/mL for DDB. At 25 µg/mL, F-α-DDB-derivative significantly inhibited migration compared with the control group, reduced Ki-67 expression, increased apoptosis, and showed stronger antitumor activity than DDB in most evaluated assays. In vivo, intraperitoneal administration of F-α-DDB-derivative (20 mg/kg, every other day for 14 days) significantly suppressed tumor growth and reduced final tumor weight compared with both the control and DDB groups. No significant abnormalities in body weight or serum biochemical markers were observed under the tested conditions.

conclusionsFluorination enhanced the antitumor activity of DDB in TNBC models. F-α-DDB-derivative represents a promising fluorinated lead compound for further preclinical investigation.

Indexed as

Antineoplastic AgentsBiphenyl CompoundsTriple Negative Breast NeoplasmsAnimalsApoptosisCell Line, TumorCell MovementCell ProliferationCell SurvivalFemaleHumansKi-67 AntigenMiceMice, NudeXenograft Model Antitumor AssaysAntineoplastic AgentsbifendateBiphenyl CompoundsKi-67 AntigenAntitumor activityBifendateF-α-DDB-derivativePreclinical studyTriple-negative breast cancerXenograft

Identifiers

PMID42286551

DOI10.1186/s12885-026-16335-1

PMCPMC13628923

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.