Drug intelligence / Profile preview

6-bromopurine

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

6-Bromopurine is a synthetic halogenated purine derivative and nucleoside analogue. It is primarily used as an intermediate in organic synthesis and chemical research. Studies have shown that it can inhibit tumor growth when combined with azaserine, likely by blocking guanine nucleotide biosynthesis between inosine 5'-phosphate and guanosine 5'-phosphate. This compound enhances the carcinostatic activity of azaserine in certain cancer cell models (e.g., sarcoma 180 and Ehrlich carcinoma). Additionally, its nucleosides are excellent substrates for substitution reactions with N-, O-, and S-containing nucleophiles in polar solvents. In preclinical studies, radiolabeled forms of 6-halogenopurines (including 6-bromopurine) have been explored as pro-probes for positron emission tomography to monitor multidrug resistance-associated protein function due to their ability to cross the blood-brain barrier and form glutathione conjugates exported by ATP-dependent transporters[1][2][5][7].

Other names
6-bromo-1H-purine6-bromo-9H-purinePurine, 6-bromo-BROMOPURINE
02

Targets

NDT (Nucleoside 2-deoxyribosyltransferase)

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