title: Synthetic Entries to and Biological Activity of Pyrrolopyrimidines.
abstract: This review summarizes recent literature (2000-2015) on the synthesis and pharmaceutical properties of pyrrolopyrimidines. These modified pyrimidine bases, fused to a pyrrole ring, and their corresponding nucleosides display a broad applicability in medicinal chemistry. This overview is divided into three main sections, according to the respective isomers: pyrrolo[2,3-d]pyrimidines, pyrrolo[3,2-d]pyrimidines, and pyrrolo[3,4-d]pyrimidines. Each section contains a description of common retro-synthetic strategies, with particular attention for newly reported synthetic entries to the scaffold. Next, the synthetic strategies and the ways in which the scaffolds can be further modified are exemplified according to the biological properties of the obtained products.
authors.affiliation: Department of Sustainable Organic Chemistry and Technology, Ghent University , Coupure links 653, B-9000 Ghent, Belgium.
authors.forename: Laurens M
authors.initials: LM
authors.lastname: De Coen
authors.affiliation: Department of Sustainable Organic Chemistry and Technology, Ghent University , Coupure links 653, B-9000 Ghent, Belgium.
authors.forename: Thomas S A
authors.initials: TS
authors.lastname: Heugebaert
authors.affiliation: Department of Sustainable Organic Chemistry and Technology, Ghent University , Coupure links 653, B-9000 Ghent, Belgium.
authors.forename: Daniel
authors.initials: D
authors.lastname: García
authors.affiliation: Department of Sustainable Organic Chemistry and Technology, Ghent University , Coupure links 653, B-9000 Ghent, Belgium.
authors.forename: Christian V
authors.initials: CV
authors.lastname: Stevens
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D055808:Drug Discovery / Q000379:methods; D006801:Humans; D008958:Models, Molecular; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011743:Pyrimidines; D011758:Pyrroles; C527741:pyrrolopyrimidine