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硼簇药效团修饰的腺嘌呤核苷和 2'-脱氧腺嘌呤核苷作为新型人血小板功能调节剂。

Adenosine and 2'-deoxyadenosine modified with boron cluster pharmacophores as new classes of human blood platelet function modulators.

机构信息

Institute for Medical Biology, Polish Academy of Sciences, Łódź, Poland.

出版信息

ChemMedChem. 2010 May 3;5(5):749-56. doi: 10.1002/cmdc.201000075.

Abstract

Novel types of adenosine and 2'-deoxyadenosine derivatives containing boron clusters at positions C2', N6, or C8 were synthesized. The effect of these modified compounds on platelet function was studied. Modification of adenosine at the C2' position with a para-carborane cluster (C(2)B(10)H(11)) results in efficient inhibition of platelet function, including aggregation, protein secretion, and P-selectin expression induced by thrombin or ADP. These preliminary findings and the new chemistry proposed form the basis for the development of a new class of adenosine analogues that modulate human blood platelet activities.

摘要

合成了新型的腺嘌呤和 2'-脱氧腺嘌呤衍生物,其中硼簇位于 C2'、N6 或 C8 位置。研究了这些修饰化合物对血小板功能的影响。在 C2'位置用间位碳硼烷簇(C(2)B(10)H(11))修饰腺嘌呤可有效抑制血小板功能,包括凝血酶或 ADP 诱导的聚集、蛋白分泌和 P-选择素表达。这些初步发现和提出的新化学为开发调节人血小板活性的新型腺嘌呤类似物奠定了基础。

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