Exploring Human Adenosine A3 Receptor Complementarity and Activity for Adenosine Analogues Modified in the Ribose and Purine Moiety

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2005 Jan 27

PMID 15670905

Citations 8

Authors

Philippe Van Rompaey

Kenneth A Jacobson

Ariel S Gross

Zhan-Guo Gao

Serge Van Calenbergh

Affiliations

Soon will be listed here.

Abstract

In this paper we investigated the influence on affinity, selectivity and intrinsic activity upon modification of the adenosine agonist scaffold at the 3'- and 5'-positions of the ribofuranosyl moiety and the 2- and N6-positions of the purine base. This resulted in the synthesis of various analogues, that is, 3-12 and 24-33, with good hA3AR selectivity and moderate-to-high affinities (as in 32, Ki=27 nM). Interesting was the ability to tune the intrinsic activity depending on the substituent introduced at the 3'-position.

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