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Updated: Aug 5, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Guanidine-based drugs in cancer therapy
Almudena Del Campo-Balguerías1, Alberto Ocaña2, Iván Bravo3
1Universidad de Castilla-La Mancha, Departamento de Química Inorgánica, orgánica y bioquímica, Facultad de Farmacia-Centro de Innovación en Química Avanzada (ORFEO-CINQA), Unidad nanoDrug, 02008 Albacete, Spain.
Guanidine molecules are versatile nitrogen-rich compounds crucial in medicinal chemistry. This review highlights their significant role and potential in developing novel cancer therapies.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Design
Background:
- Guanidine-containing molecules are nitrogen-rich compounds with unique properties.
- Their ability to form non-covalent interactions and act as superbases makes them valuable in drug development.
- These features underpin a broad range of biomedical applications.
Purpose of the Study:
- To provide a comprehensive review of guanidine-based structures.
- To focus on the application of guanidine scaffolds in oncology.
- To cover approved drugs, clinical trial agents, and preclinical candidates.
Main Methods:
- Literature review of guanidine-containing molecules in cancer research.
- Analysis of clinically approved drugs, agents in clinical trials, and preclinical candidates.
- Integration of fundamental chemistry principles with translational oncology applications.
Main Results:
- Guanidine scaffolds are pivotal in medicinal chemistry and drug design.
- Significant number of guanidine-based compounds show promise in cancer treatment.
- The review covers a spectrum of guanidine structures from approved to preclinical agents.
Conclusions:
- Guanidine-based structures possess significant potential for innovative cancer therapeutic strategies.
- The versatility of guanidine scaffolds continues to drive advancements in oncology.
- Further research integrating chemistry and translational applications will unlock new cancer treatments.
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