title: Pyrazole related nucleosides 5. Synthesis and biological activity of 2'-deoxy-2',3'-dideoxy- and acyclo-analogues of 4-iodo-1-beta-D-ribofuranosyl-3-carboxymethyl pyrazole (IPCAR).
abstract: Continuing our studies on the structure-activity relationships (SAR) of 4-iodo-1-beta-D-ribofuranosyl-3-carboxymethyl pyrazole (IPCAR), the ribofuranosyl moiety has been substituted with acyclic chains, namely 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]-pyrazole derivatives (4, 5 and 8, 9 respectively), with the 2'-deoxy-beta-D-ribofuranosyl group (12 and 13) and finally with the 2',3'-dideoxy-D-glycero-pentofuranosyl-moiety (16 and 17). None of the new compounds display any interesting biological activity.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
authors.forename: S
authors.initials: S
authors.lastname: Manfredini
authors.forename: P G
authors.initials: PG
authors.lastname: Baraldi
authors.forename: R
authors.initials: R
authors.lastname: Bazzanini
authors.forename: E
authors.initials: E
authors.lastname: Durini
authors.forename: S
authors.initials: S
authors.lastname: Vertuani
authors.forename: A
authors.initials: A
authors.lastname: Pani
authors.forename: T
authors.initials: T
authors.lastname: Marceddu
authors.forename: F
authors.initials: F
authors.lastname: Demontis
authors.forename: L
authors.initials: L
authors.lastname: Vargiu
authors.forename: P
authors.initials: P
authors.lastname: La Colla
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D009705:Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects; D015003:Yeasts / Q000187:drug effects
chemical_list: C113917:4-iodo-1-ribofuranosyl-3-carboxymethyl pyrazole; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D009705:Nucleosides; D011720:Pyrazoles