期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 7, 页码 1470-1475出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00285
关键词
acetamidine; cancer; inducible nitric oxide synthase; inhibitor; synthesis; glioma
资金
- University G. d'Annunzio of Chieti-Pescara local grant: FAR Maccallini 2018
- University G. d'Annunzio of Chieti-Pescara local grant: FAR Cataldi 2019
- University G. d'Annunzio of Chieti-Pescara local grant: FAR Amoroso2019
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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