Non-platinum anti-cancer compounds via dissociative electron transfer
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Solution Overview
Problem
Current cancer treatments, particularly chemotherapy, face challenges due to severe toxic side effects and drug resistance, necessitating the development of less toxic anti-cancer agents with improved mechanisms of action.
Innovation Solution
Non-platinum-based anti-cancer compounds, discovered through the femtomedicine approach, which induce anti-cancer effects by undergoing dissociative electron transfer reactions in cancer cells, minimizing toxicity to normal cells and overcoming resistance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional chemotherapeutic agents are used to treat cancer, then cancer cells are killed, but severe toxic side effects occur in normal cells
Solution Approach 1:
The patent applies local quality by designing compounds that exhibit different reactivity in different cellular environments. The non-platinum-based compounds remain stable in normal cells but undergo rapid dissociative electron transfer in cancer cells, producing cytotoxic effects only where needed. This spatial differentiation of chemical reactivity resolves the contradiction between killing cancer cells and protecting normal cells from toxicity.
Solution Approach 2:
The patent employs parameter changes by utilizing the different redox potentials and electron transfer characteristics of cancer cells versus normal cells. The compounds are designed to undergo dissociative electron transfer at potentials characteristic of cancer cells, transforming from stable prodrugs to active cytotoxic agents only in the cancer cell environment. This parameter-based differentiation enables selective cancer cell killing while sparing normal cells.
2Reliability
If platinum-based anti-cancer drugs like cisplatin are used, then cancer treatment efficacy is improved, but severe toxic side effects and drug resistance develop
Solution Approach 1:
The patent applies this principle by using non-platinum-based compounds that are designed to undergo irreversible dissociative electron transfer and decompose after exerting their cytotoxic effect. Unlike platinum drugs that can accumulate and cause long-term toxicity and resistance, these compounds act as single-use agents that decompose into harmless products after killing cancer cells, eliminating the problems of accumulation-induced toxicity and resistance.
Solution Approach 2:
The patent changes the fundamental chemical parameter from platinum-based coordination chemistry to non-platinum dissociative electron transfer reactions. This parameter change eliminates the mechanisms by which platinum drugs cause toxicity (DNA crosslinking) and resistance (efflux pumps, DNA repair), as the new compounds operate through a completely different chemical mechanism that cancer cells cannot easily counteract.
3Reliability
If multiple anti-cancer agents are used in combination chemotherapy, then treatment efficacy is enhanced, but toxicity to normal cells increases
Solution Approach 1:
The patent applies universality by designing a single non-platinum-based compound that performs multiple functions: it acts as a prodrug that is stable during circulation, selectively activates in cancer cells through dissociative electron transfer, produces cytotoxic effects, and decomposes into harmless products. This multi-functionality within a single agent achieves the benefits of combination therapy (enhanced efficacy) without the cumulative toxicity of multiple agents.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds effectively kill cancer cells with minimal toxicity to normal cells, offering a targeted chemotherapy approach that reduces side effects and enhances treatment efficacy.
Implementation Method 1
Non-platinum-based anti-cancer compounds, discovered through the femtomedicine approach, which induce anti-cancer effects by undergoing dissociative electron transfer reactions in cancer cells
Data Source
AI summary
Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.