Dinuclear Gold(I) Complexes with Bridging Ligands for Cancer Treatment

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Solution Overview

Problem

There is a need for gold(I) complexes with enhanced lipophilicity and increased cellular uptake to improve their anticancer activity.

Innovation Solution

The development of dinuclear phosphane gold(I) complexes incorporating a 2-(di-tert-butylphosphino)biphenyl ligand and a bis(diphenylphosphino)alkane ligand, which are bonded to gold atoms and feature a bridging bis(diphenylphosphino)alkane ligand.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional mononuclear gold(I) complexes are used, then the structure is simple and easy to synthesize, but the lipophilicity and cellular uptake are insufficient

Engineering Contradiction:

ImprovelipophilicityVSAvoidcomplex structure

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent combines two gold(I) centers into a single dinuclear complex, bridged by a diphosphane ligand. This merging approach increases the overall lipophilicity of the complex and enhances cellular uptake, while the bridging ligand provides structural organization that prevents excessive complexity

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The complex employs a composite structure consisting of two gold(I) centers, a 2-(di-tert-butylphosphino)biphenyl ligand, and a bridging bis(diphenylphosphino)alkane ligand. This composite design allows optimization of lipophilicity through the tert-butyl groups and aromatic systems while maintaining defined structural complexity through coordinated ligand architecture

Inventive Principle:

Principle #40Composite materials

2Object-affected harmful factors

If conventional gold(I) complexes with lower cytotoxicity are used, then the side effects are reduced, but the anticancer activity is insufficient

Engineering Contradiction:

Improveanticancer activityVSAvoidcytotoxicity

Core Design Contradiction:

Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent modifies key parameters of the gold(I) complex including oxidation state (maintained at +1), coordination geometry (linear), and ligand composition (phosphane-based with specific steric and electronic properties). These parameter changes enhance anticancer activity through improved mitochondrial targeting and TrxR inhibition while the cationic nature and controlled stability profile help manage cytotoxicity

Inventive Principle:

Principle #35Parameter changes

3Ease of operation

If complexes with higher cellular uptake are developed, then the anticancer potency increases, but the structural complexity and synthesis difficulty increase

Engineering Contradiction:

Improvecellular uptakeVSAvoidsynthesis difficulty

Core Design Contradiction:

Ease of operationVSEase of manufacture

Solution Approach 1:

The patent optimizes lipophilicity parameters through selection of specific phosphane ligands containing tert-butyl groups and aromatic systems, which enhance membrane permeability and cellular uptake. The linear coordination geometry and cationic character are maintained to facilitate cellular entry while the modular ligand design allows for relatively straightforward synthesis through coordination chemistry

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250041427A1Dinuclear phosphane gold(i) complexes for treating cancer

Publication Date: 2025.02.06 KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS

AI summary

A complex for treating cancer includes a 2-(di-tert-butylphosphino)biphenyl ligand and a bis(diphenylphosphino)alkane ligand. The complex is dinuclear having two gold atoms, wherein the 2-(di-tert-butylphosphino)biphenyl ligand and the bis(diphenylphosphino)alkane ligand are bonded to the gold atoms, and wherein the bis(diphenylphosphino)alkane ligand is bridging the two gold atoms.