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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 nitrogen-rich compounds crucial for drug design. This review highlights their use in oncology, from approved drugs to preclinical 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 medicinal chemistry.
- These features are key to their wide range of biomedical applications.
Purpose of the Study:
- To provide a comprehensive review of guanidine-based structures in oncology.
- To cover clinically approved drugs, agents in clinical trials, and preclinical candidates.
- To underscore the therapeutic potential of guanidine scaffolds against cancer.
Main Methods:
- Literature review of guanidine-based compounds.
- Focus on applications in cancer treatment.
- Analysis of approved, trial-stage, and preclinical oncology drugs.
Main Results:
- Guanidine scaffolds are pivotal in medicinal chemistry and drug design.
- Significant number of guanidine-based drugs are approved or in development for cancer.
- Demonstrated versatility in targeting various cancer types.
Conclusions:
- Guanidine structures offer a promising scaffold for developing novel cancer therapeutics.
- Integrating chemistry and translational research highlights their potential.
- Continued exploration of guanidine derivatives is essential for future oncology strategies.
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