Terpenic Coumarin Derivatives for Selective Cancer Cell Targeting

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current anti-cancer agents have low selectivity, leading to significant side effects on healthy cells and a lack of definitive treatment for cancer, necessitating the development of more selective and effective compounds.

Innovation Solution

The use of terpenic coumarin-derived compounds such as 14'-acetoxybadrakemin, 14'-acetoxycolladonin, or 14'-hydroxycolladonin, or their salts, hydrates, and stereoisomers, for the treatment of various types of cancer, potentially combined with other active ingredients like anticancer agents, to enhance efficacy and reduce side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional anti-cancer agents are used, then cancer cell proliferation is inhibited, but healthy cells are also affected causing serious side effects

Engineering Contradiction:
Improveselectivity of anti-cancer agentVSAvoidside effects on healthy cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing coumarin derivatives with specific structural modifications (terpenic coumarins with particular substitution patterns) that enable selective interaction with cancer cell targets while sparing healthy cells. The molecular structure is optimized to have specific affinity for cancer cell mechanisms, achieving localized effectiveness at the molecular level.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically modifying the chemical structure of coumarin derivatives (changing R groups, substitution positions, and molecular weight parameters) to optimize the balance between cancer cell efficacy and healthy cell safety. These structural parameter adjustments enhance selectivity while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If anti-cancer agents with broader spectrum are used to treat multiple cancer types, then treatment coverage is improved, but selectivity and reduced side effects are compromised

Engineering Contradiction:
Improvetreatment coverage for multiple cancer typesVSAvoidselectivity of anti-cancer agent
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent achieves universality by developing coumarin derivative compounds that demonstrate broad-spectrum anti-cancer activity across multiple cancer types (colorectal, breast, lung, pancreatic, prostate cancers) while maintaining a consistent mechanism of action. The core coumarin structure provides universal applicability, with specific substituents fine-tuning the activity profile for different cancer types.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP3784230B1The use of terpenic coumarine derivative molecules in the treatment of cancer disease
Publication Date: 2022.11.30 T C ISTANBUL MEDIPOL UNIVERSITESI
  • EP3784230B1 patent drawing
  • EP3784230B1 patent drawing
  • EP3784230B1 patent drawing

AI summary

The present invention relates to compounds suitable for use in the treatment of cancer disease and to pharmaceutical compositions comprising said compounds.