Phosphine Transition Metal Complex for Anticancer Use

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Solution Overview

Problem

Conventional phosphine transition metal complexes, such as those previously proposed by the applicant, have low solubility in water, limiting their administration forms and potentially impairing their anticancer effect.

Innovation Solution

A novel phosphine transition metal complex with improved solubility in aqueous solvents is developed, represented by formula (1), where R1 to R10 are optionally substituted alkyl or cycloalkyl groups, and M is a transition metal atom like gold, copper, or silver, allowing for enhanced solubility and production methods involving phosphine derivatives and transition metal salts.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a phosphine transition metal complex is used as an anticancer agent, then anticancer activity is achieved, but solubility in water is low

Engineering Contradiction:

Improveanticancer activityVSAvoidsolubility in water

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the molecular structure parameters of the phosphine transition metal complex by introducing specific substituents (R1-R10 groups) and adjusting the coordination geometry, thereby changing the physical chemical properties to improve water solubility while maintaining anticancer activity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite structure by combining phosphine ligands with transition metal atoms (Au, Cu, Ag) to form a new complex compound that exhibits both anticancer activity and improved solubility properties through the synergistic effect of its components

Inventive Principle:

Principle #40Composite materials

2Reliability

If low solubility phosphine transition metal complex is administered to living body, then anticancer effect is achieved, but deposition occurs in body and administration form is limited

Engineering Contradiction:

Improveanticancer effectVSAvoidadministration form

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

By changing the solubility parameter of the complex through molecular structure modification, the patent enables the drug to be administered in multiple forms (intravenous, oral, intraperitoneal) without causing deposition, thereby expanding the range of administration forms

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS11180516B2Phosphine transition metal complex, method for producing same, and anticancer agent

Publication Date: 2021.11.23 NIPPON CHEMICAL IND CO LTD

AI summary

The phosphine transition metal complex of the present invention is represented by formula (1).Preferably, R1 and R6 are identical groups, R2 and R7 are identical groups, R3 and R8 are identical groups, R4 and R9 are identical groups, R5 and R10 are identical groups, and n and y are identical numbers. The phosphine transition metal complex is suitably obtained by reacting a phosphine derivative represented by formula (2) and a phosphine derivative represented by formula (3) with a salt of a transition metal of gold, copper or silver.See the description for the meanings of the symbols in each formula.