Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage |
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| Authors: | Galli Ubaldina Ercolano Emanuela Carraro Lorenzo Blasi Roman Cintia R Sorba Giovanni Canonico Pier Luigi Genazzani Armando A Tron Gian Cesare Billington Richard A |
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| Affiliation: | Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center Università degli Studi del Piemonte Orientale A. Avogadro, Via Bovio 6, 28100 Novara, Italy. |
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| Abstract: | One of the great challenges of medicinal chemistry is to create novel, effective, chemotherapeutic agents that show specificity for cancer cells combined with low systemic toxicity. A novel idea is to target the enzymes of the NAD biosynthesis and recycling pathways given that cancer cells display a higher NAD turnover rate than healthy cells. To this end, the compound FK866 (APO866; (E)-N-[4-(1-benzoylpiperidin-4-yl) butyl]-3-(pyridin-3-yl) acrylamide), which blocks nicotinamide phosphoribosyltransferase (NMPRTase) has entered clinical trials as a potential chemotherapeutic agent. Here we report the synthesis of analogues of FK866 synthesized by click chemistry. |
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| Keywords: | bioisostere chemotherapeutic agent click chemistry FK866 NAD triazole |
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