Formula (I) Anticancer Conjugates for Reduced Normal-Cell Toxicity
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Solution Overview
Problem
Existing anti-cancer compounds are often toxic to normal cells and ineffective at tolerable doses, necessitating the development of new compounds with improved efficacy and reduced toxicity for treating various cancers.
Innovation Solution
Development of compounds of Formula (I) and their derivatives, which can be administered in compositions for treating diseases, including cancer, through various routes, and synthesized using specific reaction methods involving disulfides and thiol reducing agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing anti-cancer compounds are used to treat cancer, then anti-cancer activity is achieved, but toxicity to normal cells increases
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of existing anti-cancer compounds through systematic variation of R1, R2, R3, R4, R5, R6, and R7 substituents. These structural parameter changes aim to optimize the balance between anti-cancer efficacy and toxicity profile by exploring different molecular configurations while maintaining core pharmacological activity.
Solution Approach 2:
The patent employs composite material principles by creating conjugates that combine anti-cancer compounds with carrier molecules or functional groups. This composite approach allows the drug molecule to be coupled with structures that enhance selective delivery to tumor cells while reducing off-target toxicity to normal cells.
2Reliability
If existing anti-cancer compounds are used at higher doses to improve efficacy, then anti-cancer activity increases, but toxicity to normal cells increases
Solution Approach 1:
The patent uses parameter changes to optimize the dose-response relationship by modifying molecular properties such as solubility, stability, and bioavailability through substituent variations. These changes enable the compounds to achieve therapeutic efficacy at lower, less toxic doses by improving pharmacokinetic parameters.
Solution Approach 2:
The patent applies local quality principles by introducing functional groups or substituents at specific positions (R1 through R7) that enhance selective accumulation in tumor tissue. This localized modification allows the compound to concentrate anti-cancer activity where needed while minimizing systemic exposure and toxicity to normal cells.
Data Source
AI summary
Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating. Further embodiments include methods for making the inventive compound. Additional embodiments of the invention are also discussed herein.