Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.

ACS Medicinal Chemistry Letters
Cristina MaccalliniRosa Amoroso

Abstract

Nitric oxide is an important inflammation mediator with a recognized role in the development of different cancers. Gliomas are primary tumors of the central nervous system with poor prognosis, and the expression of the inducible nitric oxide synthase correlates with the degree of malignancy, changes in vascular reactivity, and neo-angiogenesis. Therefore, targeting the nitric oxide biosynthesis appears as a potential strategy to impair glioma progression. In the present work a set of aryl and amido-aryl acetamidine derivatives were synthesized to obtain new potent and selective inducible nitric oxide synthase inhibitors with improved physicochemical parameters with respect to the previously published molecules. Compound 17 emerged as the most promising inhibitor and was evaluated on C6 rat glioma cell line, showing antiproliferative effects and high selectivity over astrocytes.

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Citations

Aug 13, 2020·ChemMedChem·Cristina MaccalliniRosa Amoroso
Jul 5, 2021·Bioorganic & Medicinal Chemistry·Fabio AriasM Encarnación Camacho
Jul 23, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Cristina MaccalliniRosa Amoroso
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Marialucia GalloriniCristina Maccallini

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