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Molecules 2014, 19(10), 15754-15767;

Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518052, China
Author to whom correspondence should be addressed.
Received: 25 July 2014 / Revised: 22 September 2014 / Accepted: 22 September 2014 / Published: 29 September 2014
(This article belongs to the Section Medicinal Chemistry)
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Nicotinamide adenine dinucleotide (NAD), one of the most important coenzymes in the cells, is a substrate of the signaling enzyme CD38, by which NAD is converted to a second messenger, cyclic ADP-ribose, which releases calcium from intracellular calcium stores. Starting with 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamide adenine dinucleotide (ara-F NAD), a series of NAD analogues were synthesized and their activities to inhibit CD38 NAD glycohydrolase (NADase) were evaluated. The adenosine-modified analogues showed potent inhibitory activities, among which 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamide guanine dinucleotide (ara-F NGD) was the most effective one. The structure-activity relationship of NAD analogues was also discussed. View Full-Text
Keywords: synthesis; NAD analogues; CD38; inhibitors synthesis; NAD analogues; CD38; inhibitors

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Wang, S.; Zhu, W.; Wang, X.; Li, J.; Zhang, K.; Zhang, L.; Zhao, Y.-J.; Lee, H.C.; Zhang, L. Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase. Molecules 2014, 19, 15754-15767.

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