Synthesis and calcium mobilization activity of cADPR analogues which integrate nucleobase, northern and southern ribose modifications |
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Authors: | Zhou Yue Yu Peilin Jin Hongwei Yang Zhenjun Yue Jianbo Zhang Liangren Zhang Lihe |
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Affiliation: | State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. |
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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. |
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