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Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity
Rocío Recio1, Patricia Lerena1, Esther Pozo1
1Departamento de Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Profesor García González, 2, 41012 Sevilla, Spain.
Journal of Medicinal Chemistry
|July 8, 2021
Summary
Researchers developed novel carbohydrate-based Neurokinin-1 Receptor (NK1R) antagonists with broad-spectrum anticancer activity. Compound 14α, a galactosyl derivative, shows significant NK1R antagonism and selective cytotoxicity against multiple cancer cell lines.
Area of Science:
- Medicinal Chemistry
- Oncology
- Carbohydrate Chemistry
Background:
- Neurokinin-1 Receptor (NK1R) antagonists show promise in cancer treatment.
- Developing novel anticancer agents with high selectivity is crucial.
Purpose of the Study:
- To synthesize and evaluate carbohydrate-based NK1R antagonists as potential anticancer agents.
- To identify specific compounds with potent and selective cytotoxic activity.
Main Methods:
- Synthesis of novel compounds derived from d-galactose and l-arabinose.
- Evaluation of NK1R antagonistic activity and binding affinity.
- Assessment of broad-spectrum anticancer activity against various cancer cell lines.
Main Results:
- All synthesized compounds demonstrated high affinity and NK1R antagonistic activity.
- Compounds exhibited broad-spectrum anticancer activity and selectivity comparable to Cisplatin.
- Galactosyl derivative 14α showed significant NK1R antagonist effect and high binding affinity (IC50 = 50.4 nM, Ki = 22.4 nM).
- Compound 14α displayed marked selective cytotoxic activity against 12 cancer cell lines.
Conclusions:
- Carbohydrate-based NK1R antagonists represent a promising strategy for cancer therapy.
- Compound 14α is a potent and selective NK1R antagonist with significant anticancer potential.
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