US 12150935 B1Patent grantUnited States

Fluorinated Compound for Cancer Cell Screening

Official patent title

3-(3-(1,3-dioxoisoindolin-2-yl) propyl)-5-(4-fluorobenzylidene) thiazolidine-2,4-dione as a potential antitumor and apoptotic inducer

Arabic title: 3-(3-(1,3-ديوكسوإيزوإندولين-2-يل)بروبيل)-5-(4-فلوروبنزيليدين)ثيازوليدين-2,4-ديون بوصفه عاملًا محتملًا مضادًا للأورام ومحفزًا للاستموات

Invention

Problem

Current cancer treatments can damage healthy tissue and may produce serious adverse effects, while malignant cells can evade programmed cell death. New, well-characterized compounds are needed for preclinical evaluation as cytotoxic and apoptosis-inducing candidates.

Why it matters

A compound with a defined synthesis and measured activity across several cancer cell lines can provide a starting point for medicinal-chemistry and mechanism studies. The reported results remain in vitro and do not establish treatment in patients.

Approach

The disclosure prepares a specific fluorobenzylidene thiazolidinedione derivative by reacting a thiazolidinedione precursor with 4-fluorobenzaldehyde in a polar protic solvent with acid and piperidine, then applies the compound to cancer cells to investigate cytotoxicity and apoptosis-related pathways.

Who may benefit

Potential beneficiaries include oncology and apoptosis researchers, medicinal-chemistry groups, preclinical screening laboratories, and pharmaceutical teams evaluating new small-molecule leads.

Potential value

The patent links a structurally defined compound and an 80–85% claimed synthesis yield with in-vitro growth-inhibition data for multiple cancer cell lines and specified apoptosis-related pathways, creating a documented package for further lead validation.

Background

Cancer progression involves uncontrolled cell growth and can include disruption of apoptosis, the regulated process that removes damaged or unnecessary cells. Existing treatment options include surgery, radiation, chemotherapy, and newer targeted combinations, but efficacy and toxicity remain important limitations. The patent focuses on a thiazolidinedione derivative intended to reduce cancer-cell numbers and induce apoptosis. It discusses p53, BAX, caspase, BCL-2, MMP2, and MMP9 pathways and reports testing against several established human cancer cell lines.

Technology overview

The compound is synthesized by refluxing the specified thiazolidinedione precursor and 4-fluorobenzaldehyde for 6–10 hours in a polar protic solvent with acetic acid and piperidine in some embodiments. The patent reports 80–85% yield and in-vitro growth inhibition at 100 μg/mL in A549, HCT116, PC3, FaDu, MDA-MB-468, and HeLa cells, alongside a normal oral epithelial cell line. Claims cover cytotoxic contact, apoptosis pathways, synthesis, carriers, and dosage-form options.

Potential applications

In-vitro screening of a thiazolidinedione anticancer candidate.
Research on apoptosis-related p53, BAX, caspase, BCL-2, MMP2, and MMP9 pathways.
Medicinal-chemistry lead optimization and structure–activity studies.
Preclinical formulation research with pharmaceutically acceptable carriers.

Evidence-supported advantages

Uses a structurally defined small molecule with a specified preparation route.
Reports an 80–85% synthesis yield in claimed embodiments.
Provides in-vitro growth-inhibition data across six cancer cell lines.
Links the proposed activity to several apoptosis-related molecular pathways.

Development stage

Compound synthesis and in-vitro cancer-cell testing are described; clinical efficacy, safety, and commercialization were not established.

Commercial opportunity

The compound may be considered for licensing or sponsored research as an early oncology lead. Any development program would require confirmation of selectivity and mechanism, pharmacology, toxicology, formulation, in-vivo efficacy, and clinical evaluation before therapeutic use could be considered. Early comparison with reference compounds would guide prioritization.

Patent classifications

WIPO IPC

A61K31/427Preparations for medical, dental or toiletry purposes
A61P35/00Specific therapeutic activity of chemical compounds or medicinal preparations

CPC

A61P35/00Specific therapeutic activity of chemical compounds or medicinal preparations
A61K31/427Preparations for medical, dental or toiletry purposes

Inventors

First inventorTarek Ahmed Yousef
InventorSaad Shaaban
InventorAhmed A. Al-Karmalawy
InventorAyman Abo Elmaaty

Keywords

thiazolidinedione
anticancer candidate
apoptosis
cytotoxicity
cancer cell lines
p53
caspase
medicinal chemistry

Patent document and drawings

The patent publication is mapped to this record. Patent drawings remain within that publication; no separately cleared public media package has been supplied.