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- Title
Synthesis and Calcium Mobilization Activity of cADPR Analogues Which Integrate Nucleobase, Northern and Southern Ribose Modifications.
- Authors
Yue Zhou; Peilin Yu; Hongwei Jin; Zhenjun Yang; Jianbo Yue; Liangren Zhang; Lihe Zhang
- Abstract
Novel cADPR mimics, which integrate nucleobase, northern and southern ribose modifications were synthesized. The key steps of the synthesis were a Cu(I)-catalyzed Hüisgen [3+2] cycloaddition and a microwave-assisted intramolecular pyrophosphorylation. Preliminary biological investigations showed that these cADPR mimics are membrane-permeating agonists of the calcium signaling pathway. The introduction of chlorine or fluorine at the 2'-position of the southern riboses led to a decrease of activity. The existence of a hydrophobic group on the 3'-OH of the southern riboses does not obviously alter the agonistic activity.
- Subjects
RIBOSE; PHOSPHORYLATION; CALCIUM antagonists; HYDROPHOBIC surfaces; CHEMICAL reactions; CHLORINE
- Publication
Molecules, 2012, Vol 17, Issue 4, p4343
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules17044343