Nitrogen Polycyclic Aromatic Compound for Low-Toxicity Anti-Tumor Therapy

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Solution Overview

Problem

Current antitumor drugs like cisplatin have broad-spectrum efficacy but are associated with significant toxicity and drug resistance, necessitating the development of new, low-toxicity, high-efficiency therapeutic agents.

Innovation Solution

A nitrogen-containing polycyclic aromatic compound with a specific structure, shown in Formula I, is developed, which demonstrates excellent broad-spectrum anti-tumor activity and lower toxicity compared to cisplatin, and is synthesized through a method involving reactants and acid catalysts under controlled conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cisplatin is used as an anti-tumor drug, then broad-spectrum anti-tumor activity is achieved, but severe toxicity and drug resistance occur

Engineering Contradiction:
Improveanti-tumor activityVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of cisplatin by replacing the platinum center with organic compounds containing nitrogen-containing polycyclic aromatic rings, altering the fundamental parameters of the drug molecule to achieve similar anti-tumor activity with reduced toxicity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite organic molecules combining multiple polycyclic aromatic rings with nitrogen atoms, forming a complex structure that mimics the therapeutic effect of cisplatin while avoiding its toxic side effects through different chemical composition

Inventive Principle:
Principle #40Composite materials

2Reliability

If cisplatin is used to treat advanced tumors, then broad-spectrum efficacy is achieved, but drug resistance develops

Engineering Contradiction:
Improveanti-tumor efficacyVSAvoiddrug resistance
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

By changing the core metal center to organic nitrogen-containing structures, the patent creates drugs with different mechanisms of action that can overcome resistance developed to traditional platinum-based therapies

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If new anti-tumor drugs are developed to reduce toxicity, then safety is improved, but anti-tumor activity may be compromised

Engineering Contradiction:
Improvetoxicity to normal cellsVSAvoidanti-tumor activity
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent introduces specific functional groups and substituents at particular positions on the polycyclic aromatic rings to optimize the balance between anti-tumor activity and toxicity, creating localized chemical features that enhance therapeutic selectivity

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20240140950A1NITROGEN-CONTAINING POLYCYCLIC AROMATIC COMPOUND, and PREPARATION METHOD AND APPLICATION THEREOF
Publication Date: 2024.05.02 HEBEI UNIV OF SCI & TECH
  • US20240140950A1 patent drawing
  • US20240140950A1 patent drawing
  • US20240140950A1 patent drawing

AI summary

The present application provides a nitrogen-containing polycyclic aromatic compound and its preparation method and application. The nitrogen-containing polycyclic aromatic compound has a structure of Formula I, has an excellent broad-spectrum anti-tumor activity, and shows an inhibitory activity comparable to cisplatin on cervical cancer cells, breast cancer cells, melanoma cells, lung cancer cells and myeloma cells. Compared with cisplatin, the compound also has lower toxicity, and may be used as a lead compound for the development of new anti-tumor drugs.