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Literature DB >> 25522820

Diversity oriented synthesis and IKK inhibition of aminobenzimidazole tethered quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines.

Sureshbabu Dadiboyena¹, Aïcha Arfaoui², Hassen Amri², F Javier Piedrafita³, Adel Nefzi⁴.

Abstract

The derivatization of resin-bound aminobenzimidazole toward the parallel solid-phase synthesis of aminobenzimidazole tethered pharmacologically important heterocycles such as quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines is reported. All the compounds were tested for IKK inhibition. Only one compound elicited significant inhibition of IKKε, TBK-1 and IKK2.

Entities: Chemical Disease Gene Species

Keywords: 1,3-Dipolar cycloaddition; Aminobenzimidazoles; Benzodiazepinetriones; Heterocycles; Intramolecular cyclization; Isoxazoles; Isoxazolines; Quinazolinediones; Solid-phase synthesis; Thioxoquina-zolinones

Mesh：

Substances：

Year: 2014 PMID： 25522820 PMCID： PMC4311523 DOI： 10.1016/j.bmcl.2014.11.078

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Diversity oriented synthesis and IKK inhibition of aminobenzimidazole tethered quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines.

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